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HomeMy WebLinkAboutPinney Associates Letter Page 1 of 128 The Abuse Potential of 7- Hydroxymitragynine (7-OH) According to the 8 Factors of the Controlled Substances Act Developed for Submission to the Drug Enforcement Administration (DEA), Food and Drug Administration (FDA), and National Institute on Drug Abuse (NIDA) Jack E. Henningfield, Daniel W. Wang, Mark A. Sembower, Steve Pype, Floe Foxon September 29, 2025 Page 2 of 128 Table of Contents Table of Contents ............................................................................................................ 2 List of Abbreviations ........................................................................................................ 4 1 Introduction .............................................................................................................. 6 2 Factor 1: Actual or Relative Potential for Abuse ....................................................... 9 2.1 Pharmacology ................................................................................................... 9 2.2 Nonclinical Abuse Potential Models (Rewarding Effects) ................................ 11 2.2.1 Self-Administration ................................................................................... 11 2.2.2 Intracranial Self-Stimulation ..................................................................... 11 2.2.3 Drug Discrimination ................................................................................. 11 2.2.4 Conditioned Place Preference ................................................................. 12 2.3 Clinical Studies and Evidence of Abuse Potential in Humans ......................... 12 2.4 Implications for Abuse Potential ...................................................................... 12 3 Factor 2: Scientific Evidence of its Pharmacological Effects .................................. 13 3.1 Mechanism of Action and Opioid Binding ....................................................... 13 3.2 Effects on Other Neurotransmitter Systems .................................................... 14 3.3 Antinociception ................................................................................................ 14 3.4 Respiratory Depression .................................................................................. 14 3.5 Comparison to Morphine ................................................................................. 15 3.6 Implications for Abuse Potential ...................................................................... 15 4 Factor 3: Current State of Scientific Knowledge ..................................................... 16 4.1 Pharmacokinetics ............................................................................................ 16 4.2 Mitragynine Pseudoindoxyl ............................................................................. 18 4.3 Conclusions .................................................................................................... 18 5 Factors 4, 5, and 6: History and Current Patterns of Abuse; The Scope, Significance and Duration of Abuse; What, if any, Risk is there to the Public Health .... 19 5.1 Factor 4: History and Current Patterns of Abuse ............................................ 19 5.1.1 Reasons for Use ...................................................................................... 20 5.1.2 Dosing, Routes of Administration, and Trajectory of Use......................... 20 5.2 Factor 5: Scope, Duration, and Significance of Abuse .................................... 21 5.2.1 National Surveillance Systems ................................................................ 21 5.2.2 Published Case Reports .......................................................................... 26 5.2.3 Social Media Discussion .......................................................................... 26 5.3 Factor 6: What, if any, Risk is there to the Public Health ................................ 30 Page 3 of 128 5.3.1 Pharmacological Risks............................................................................. 31 5.3.2 Abuse, Dependence, and Withdrawal Risk .............................................. 31 5.3.3 Potential Benefits to Consumers and Public Health ................................. 32 5.4 Implications ..................................................................................................... 32 6 Factor 7: The Psychic or Physiological Dependence Liability ................................ 33 7 Factor 8: Whether the Substance is an Immediate Precursor of a Substance Already Controlled ......................................................................................................... 34 8 Scheduling Recommendation ................................................................................ 34 8.1 Policy Implementation Considerations to Minimize Unintended Consequences 35 9 Research Priorities and Policy Considerations ...................................................... 36 9.1 Comparison of 7-OH to Kratom and other Substances ................................... 39 9.2 Potential Unintended Consequences of Schedule I Placement and Policy Implications ................................................................................................................ 40 9.2.1 Potential Unintended Consequences of Scheduling ................................ 40 10 References ......................................................................................................... 43 11 Appendices ......................................................................................................... 52 11.1 Appendix 1: Published Findings Related to Abuse, Physical Dependence, Withdrawal, and Safety Signals of 7-OH .................................................................... 52 11.2 Appendix 2: Press Release: FDA Takes Steps to Restrict 7-OH Opioid Products Threatening American Consumers ............................................................. 73 11.3 Appendix 3: FDA Report: 7-Hydroxymitragyine (7-OH): An Assessment of the Scientific Data and Toxicological Concerns Around an Emerging Opioid Threat ...... 75 11.4 Appendix 4: FDA Slide Set: Preventing The Next Wave of the Opioid Epidemic: What You Need to Know About 7-OH ...................................................................... 100 11.5 Appendix 5: Department of Health and Human Services Press Conference Transcript ................................................................................................................. 106 11.6 Appendix 6: Dr. Martin A. Makary 7-OH Letter to Colleagues ....................... 128 Page 4 of 128 List of Abbreviations Abbreviation Definition Β-arrestin-2 Beta (β)-arrestin-2 7-OH (7-OH-MG, 7-OH-MIT) 7-hydroxymitragynine 8-FA 8-Factor Analysis CAMU Commonly Accepted for Medical Use CNS Central nervous system CPP Conditioned place preference CSA Controlled Substances Act CYP Cytochrome P450 (i.e., 3A, 2D6, 3A4) DAWN Drug Abuse Warning Network DEA Drug Enforcement Agency DHHS Department of Health and Human Services DOJ Department of Justice DOR Delta (δ)-opioid receptor ECDD World Health Organization's Expert Committee on Drug Dependence FAERS Food and Drug Administration Adverse Event Reporting System FDA Food and Drug Administration GI Gastrointestinal IC50 Half-maximal inhibitory concentration ICSS Intracranial self-stimulation IP intraperitoneal IQR Interquartile range IV intravenous Ki Inhibitor constant KOR Kappa (κ)-opioid receptor LSD Lysergic acid diethylamide MOR Mu (µ)-opioid receptors NDIN New Dietary Ingredient Notification NFLIS National Forensic Laboratory Information System NIDA National Institute on Drug Abuse NIH National Institutes of Health NFLIS National Forensic Laboratory Information System NPDS National Poison Data System NSDUH National Survey on Drug Use and Health PO Per oral TEDS Treatment Episodes Data Set UGT UDP-glucuronosyltransferase (i.e., UGT1A1, UGT1A3, UGT1A9) UNODC United Nations Office on Drugs and Crime U.S. United States Page 5 of 128 Disclosure This report was funded without restrictions by the Center for Plant Science and Health (CPSH). CPSH had no input into the writing of this report, its methods, or its conclusions. Through Pinney Associates, JEH, DWW, MS, SP, and FF consult to CPSH. In addition to CPSH, in the last 36 months, Pinney Associates has consulted to the Holistic Alternative Recovery Trust, NP Pharma, and Botanic Tonics LLC (the last uncompensated) on kratom science and regulatory issues and studies. Through Pinney Associates, in support of CPSH, JH has commented on kratom pharmacology, public health, and regulatory needs for state hearings and for a judicial hearing to address questions raised by the court on these same matters. JEH has also developed reports and given depositions addressing kratom addictiveness, and risks and benefits to kratom users, along with regulatory needs on behalf of several defendants in kratom litigation. Acknowledgements The authors are grateful for the care and efforts of Megan S. Harris in the editing and formatting of the report. Page 6 of 128 1 Introduction On July 29, 2025, the United States (U.S.) Food and Drug Administration (FDA) presented its assessment of a potential “novel, emerging public health threat”, 7- hydroxymitragynine (also known as 7-OH), a psychoactive substance that naturally occurs as a minor constituent of the kratom plant (Mitragyna speciosa) and also forms in the body as a metabolite of mitragynine, the plant's primary alkaloid. This assessment, shared as a news release on the FDA website (FDA, 2025a), was based on epidemiological findings and scientific data on toxicological concerns. FDA’s release linked to a summary scientific evaluation developed by FDA scientists titled “Assessment of the Scientific Data and Toxicological Concerns Around an Emerging Opioid Threat” (Reissig et al., 2025), a slide set titled “Preventing the Next Wave of the Opioid Epidemic: What You Need to Know about 7-OH” (FDA, 2025b), and a Dear Colleagues letter by Commissioner Dr. Marty Makary (2025). Additionally, the Secretary of Health and Human Services, Robert F. Kennedy, Jr., hosted a press conference described as “measures to safeguard American public from dangerous opioid 7-OH (DHHS, 2025b). Participants included Secretary Kennedy, Department of Health and Human Services (DHHS) Deputy Secretary Jim O’Neill, FDA Commissioner Dr. Marty Makary, U.S. Senator Markwayne Mullin (R-OK), and Melody Woolf (chronic pain survivor) (DHHS, 2025a). These scientific analyses and announcements summarized FDA’s findings that 7-OH binds to morphine opioid receptors (also referred to as “mu (µ)- opioid receptors or MOR”) with potentially strong effects similar to those that can be produced by morphine and other classical opioids. Of particular concern to FDA is the increasing proliferation of products that contain highly concentrated, often semi-synthetically derived 7-OH. These novel products deliver significantly higher levels of 7-OH than occur naturally or are found in traditional kratom leaf products. In its July 29, 2025 media release FDA cites evidence from key studies and assays typically considered in drug scheduling determinations, including rewarding effects in animal studies, physical dependence and withdrawal symptoms, respiratory depression (at least when administered intravenously), and effects in animals generalized to morphine. Additionally, FDA cites clinical presentations (often referred to as anecdotal reports) and receptor binding profiles. These data support FDA’s characterization of 7-OH as a substance with a pharmacological profile that is qualitatively similar to classical opioids with effects such as “euphoria, sedation, respiratory depression, and opioid-like withdrawal syndromes, with users acknowledging its significant addiction potential (Reissig et al., 2025, p. 4). FDA concluded “The pharmacological profile, abuse liability, and emerging patterns of nonmedical use establish 7-OH as a dangerous substance” (Reissig et al., 2025, p. 4). As discussed in Factor 8, such data suggest that 7-OH meets the statutory definition of an opioid as described in the 1970 Controlled Substances Act (CSA). Although some kratom products have likely been boosted in their 7-OH concentrations in the past, the widespread marketing and consumption of concentrated 7-OH products has emerged nationwide in just the past few years. FDA itself noted a clear “distinction” between kratom and kratom products that “have been used for centuries in both Page 7 of 128 medicinal and recreational settings” containing naturally low occurring levels of 7-OH compared to what the agency described as the recent widespread appearance of “7-OH opioid products” (e.g., FDA (2025a). FDA emphasized that “7-OH is found in trace amounts in the kratom plant leaf. But this is not our focus. Our primary concern is the concentrated form of 7-OH. This is an important distinction. These concentrated 7-OH opioid products are far more dangerous than traditional kratom leaf products” (Makary, 2025) Currently, many kratom and related products, including concentrated 7-OH products are marketed as dietary ingredients and/or supplements, though to date no New Dietary Ingredient Notification (NDIN) has been accepted by FDA and the lack of adequately documented history of use prior to 1994 has precluded its acceptance as an ‘old dietary ingredient’ that is exempt from the NDIN requirements as described in the 1994 Dietary Supplement Health and Education Act (DSHEA). During the FDA’s July 29, 2025, press conference, the DHHS leadership indicated that the Department would recommend the Drug Enforcement Administration (DEA) place 7- OH in the CSA. If DEA concurs, then 7-OH would be placed in Schedule I, along with heroin, LSD, and marijuana as that is the only CSA schedule for substances with high abuse potential and which are not “Commonly Accepted for Medical Use” (CAMU). CAMU is typically determined by FDA’s approval as a drug for medical use, or in a rare recent case with respect to marijuana, a substantial body of medical use, state-level authorization, and clinical evidence was considered adequate to support the designation of marijuana as CAMU despite the absence of FDA formal therapeutic/medical approval (DHHS, 2023a; DEA, 2024). Permanent placement in Schedule I requires an 8-factor analysis (8-FA), which is the structured evaluation described in the CSA that is determinative of CSA control and scheduling. Factors 1, 2, 3, and 7 are based on chemical, pharmacological, and clinical studies, while Factors 4, 5, and 6 determine public health impact and whether the substance poses an imminent hazard to public health. Factor 8 examines whether the substance is a chemical precursor of a substance that is already controlled in the CSA, or has the same chemical structure, or in the case of opioids is derived from the opium poppy by extraction, or chemical synthesis based on opium or an opium poppy constituent such thebaine or morphine or has a pharmacological profile similar to that of already controlled morphine-like opioids1. This recent action represents a shift from a 2018 DHHS decision, which rescinded a prior recommendation to schedule kratom and its alkaloids, including 7-OH. In that 1 In 21 U.S. Code § 802 – Definitions (17)The term “narcotic drug” means any of the following whether produced directly or indirectly by extraction from substances of vegetable origin, or independently by means of chemical synthesis, or by a combination of extraction and chemical synthesis: (A) Opium, opiates, derivatives of opium and opiates, including their isomers, esters, ethers, salts, and salts of isomers, esters, and ethers, whenever the existence of such isomers, esters, ethers, and salts is possible within the specific chemical designation. Such term does not include the isoquinoline alkaloids of opium. Page 8 of 128 decision, U.S. Assistant Secretary for Health Admiral Brett P. Giroir noted that the existing science did not support a recommendation to place mitragynine and 7-OH in the CSA because this would have had the effect of banning kratom product and that carried a “significant risk of immediate adverse public health consequences” if users were to switch to more lethal opioids (Giroir, 2018). Similarly, the United Nations Commission on Narcotic Drugs (UNODC) Commission on Narcotic Drugs (CND) concluded there was insufficient evidence to recommend a critical review of kratom and its alkaloids, including mitragynine and 7-OH, though it advised they be kept under surveillance (UNODC, 2021). Since then, in late August 2025, the UNODC published a warning of emerging products containing 7-OH and 7- OH’s metabolite pseudoindoxyl, recommending further educational awareness campaigns by healthcare professionals, regulators, and law enforcement, as well as enhancing surveillance, testing, detection, and epidemiological surveillance of these products. The present document provides an 8-FA of 7-OH according to the 1970 Controlled Substances Act. This 8-FA has been developed following the model laid out in FDA’s guidance, Assessment of the Abuse Potential of Drugs (FDA, 2017), while also taking into consideration the experience and evolution in approach to such assessments since the CSA was signed into law in 1970. The present analysis considered and expands upon the pharmacological and epidemiological data that were presented in FDA’s July 29, 2025 scientific assessment (Reissig et al., 2025) and incorporates insights from prior work by Pinney Associates, including the 2018 and 2022 kratom 8-FAs and related analyses (Henningfield, Fant, & Wang, 2018; Henningfield, Wang, & Huestis, 2022). The Appendices include four documents released by FDA addressing 7-OH science, warnings and educational materials (FDA, 2025a, FDA, 2025b, Makary, 2025; Reissig et al., 2025), as well as the conference transcript in Appendix 5. The purpose is to provide a structured review of the evidence typically used to inform the FDA and National Institute on Drug Abuse (NIDA) in their CSA scheduling recommendations and the DEA in its potential scheduling action, as well as to provide a resource for public health policymakers, regulators, scientists, and the public in general to learn about the risks associated with 7-OH and the complexities of its potential regulatory and legal control. This 8-FA also discusses policy considerations such as potential scheduling and enforcement approaches; efforts to mitigate unintended consequences such as fueling the formation of illicit (“black”) 7-OH markets and relapse to deadlier classical opioid use; and addressing other potential health problems and medical issues in people who found 7-OH to be more effective, acceptable or assessable than FDA approved medicines, kratom, or other approaches in addressing their health needs including opioid dependence and withdrawal. Table 1 from FDA (2017) summarizes the 8 factors of the CSA as follows: Under 21 U.S.C. 811(b) of the CSA, the medical and scientific analysis considers the following eight factors determinative of control of the drug under the CSA (21 U.S.C. 811(c)): Page 9 of 128 1. Its actual or relative potential for abuse. 2. Scientific evidence of its pharmacological effect, if known. 3. The state of current scientific knowledge regarding the drug or other substance. 4. Its history and current pattern of abuse. 5. The scope, duration, and significance of abuse. 6. What, if any, risk there is to the public health. 7. Its psychic or physiological dependence liability. 8. Whether the substance is an immediate precursor of a substance already controlled. 2 Factor 1: Actual or Relative Potential for Abuse The actual or relative potential for abuse of a substance is a primary determinant in scheduling considerations under the CSA. This factor is assessed through a combination of preclinical studies in animals and an analysis of human use patterns. For 7-OH, a number of nonclinical studies including self-administration, conditioned place preference, and drug discrimination studies indicate potential for abuse, with effects that are often comparable to, or more potent than, those of morphine. While controlled human abuse potential studies have not yet been conducted, emerging data from user reports and clinical case studies corroborate the findings from animal research, suggesting that concentrated 7-OH products are being used for their rewarding and opioid-like effects. 2.1 Pharmacology 7-OH has been shown to naturally occur at de minimis levels in the kratom plant and is generally formed in vivo from mitragynine, the parent alkaloid, through metabolic oxidation in the liver, mediated by cytochrome (CYP) P450 3A (Kruegel et al., 2019). It appears that low levels of 7-OH may also occur post-harvest in leaves by enzymatic interactions (Karunakaran, Vicknasingam, & Chawarski, 2025; Smith et al., 2024). 7-OH has demonstrated pharmacological properties consistent with potential for recreational use, abuse, and dependence. However, available evidence indicates that 7-OH acts as a partial agonist at opioid receptors, suggesting that by some measures it is weaker in its expression or less efficacious compared to morphine, such as opioid-like effects. Whether the overall abuse potential of 7-OH is most accurately described as lower, higher, or similar to morphine (the most common standard comparator) is not clear at present; however, as discussed by FDA (Reissig et al., 2025), 7-OH has sufficiently similar pharmacology to be characterized as an opioid. Moreover, although its potency (the amount of drug required to produce a given effect) varies widely across measures and studies, it requires smaller amounts of 7-OH by weight (e.g., mg) to produce a variety of abuse-related effects as compared to morphine, therefore Page 10 of 128 supporting the general description of 7-OH by FDA as a “potent’ and even “highly potent” opioid”. Specifically, 7-OH exhibits high affinity for MORs and acts as a partial agonist, producing G-protein biased signaling with limited beta- (β) arrestin-2 recruitment (Kruegel et al., 2016; Todd et al., 2020). This bias is generally associated with reduced opioid-like effects such as constipation (Gutridge et al., 2020). The FDA’s 2025 assessment characterizes 7-OH as a potent MOR agonist with high abuse potential and risk of severe dependence stating, “Critically, 7-OH produces respiratory depression, physical dependence, and withdrawal symptoms characteristic of classical opioids, such as morphine, fentanyl, oxycodone, and hydrocodone”. It is important to note that demonstrations of morphine equivalent reinforcing efficacy and respiratory depression in rodent models were by the intravenous (IV) route of administration, whereas virtually all human consumption is by the oral route. Overdose risk by the oral route would seem to be a plausible risk but has not been well- documented in animals and the evidence for apparent 7-OH attributed overdose deaths in humans is not strong. FDA described two cases in which an overdose death occurred and concluded as follows: “Although FDA’s Adverse Event Reporting System (FAERS) has documented cases reporting adverse events (13 cases, including 2 deaths) suspected to involve 7-OH, ambiguity about the contributory role of 7-OH from uncharacterized products or concomitant medications and underlying disease limits interpretation” (Reissig et al., 2025). Note that these reports are not limited to a single year but rather all the cases that have been reported to date. Whereas these reports are concerning, and this report agrees with FDA that adverse events related to 7-OH use have been under-reported, the actual numbers of such cases are very low as compared to the thousands reported over time and annually for opioids such as heroin, oxycodone and fentanyl and fentanyl related substances. Whereas most animal studies indicated that mitragynine is neither potent, strong, nor reliable in producing respiratory depression (e.g., (Henningfield, Rodricks, et al., 2022), 7-OH produced stronger morphine-like respiratory depression by the IV route at lower concentrations than mitragynine (Gonzalez et al., 2025; Harun et al., 2015). Also, unlike mitragynine, 7-OH reliably substitutes for morphine across antinociception, discrimination, and self-administration paradigms, showing dose-dependent reinforcing and conditioned place preference effects with greater potency than morphine in several animal models (Gutridge et al., 2020; Harun et al., 2015). 7-OH produces strong naloxone-reversible analgesia yet with less respiratory depression and constipation at equianalgesic doses, and exhibits higher oral bioavailability than morphine (Kruegel et al., 2016; Matsumoto et al., 2004). In mice, brain concentrations of 7-OH after mitragynine administration are sufficient to explain Page 11 of 128 most or all of the opioid-receptor mediated analgesic effects associated with mitragynine use (Kruegel et al., 2019). 2.2 Nonclinical Abuse Potential Models (Rewarding Effects) 2.2.1 Self-Administration A study by Hemby et al. (2019) evaluated the reinforcing effects of 7-OH in rats and found that 7-OH not only engendered but also maintained self-administration behavior at intravenous doses ranging from 2.5 to 10 µg/infusion, demonstrating reinforcing effects comparable to those of morphine when administered at 50 and 100 µg/infusion, suggesting 7-OH may be 10-20 times more potent than morphine in this test. In contrast, mitragynine did not maintain self-administration, highlighting a critical pharmacological distinction between the two compounds. The reinforcing effects of 7- OH were found to be mediated by both MORs and delta (δ)-opioid receptors (DOR), as intake was reduced by antagonists for both receptor types (NLXZ and NTI, respectively). This contrasts with morphine, whose reinforcing effects in the same study were primarily mediated by MORs. To contextualize these findings for human risk, an allometric scaling factor can be used to estimate a human equivalent dose. Based on the rat data, the reinforcing intravenous dose of 7-OH for a 70 kg person is estimated to be between 0.161 and 0.322 mg, compared to 1.61 mg for morphine. This calculation suggests that 7-OH might be between 5-10x more potent than morphine in producing reinforcing effects, a key indicator of abuse potential though this should be considered a possibility to be tested and not an established fact. It is crucial to note, however, that the clinical meaningfulness of such estimates is not clear because the animal data are based on intravenous administration, whereas human consumption of 7-OH products is typically oral. The abuse potential of 7-OH in humans has not been directly evaluated in human abuse potential studies by any route of administration using protocols recommended by FDA in its 2017 Guidance (FDA, 2017) nor have other potential effects of 7-OH administration been well characterized in controlled clinical studies. 2.2.2 Intracranial Self-Stimulation In an intracranial self-stimulation (ICSS) study, neither mitragynine nor 7-OH-MG showed evidence of brain rewarding effects, whereas morphine robustly and dose dependently decreased the stimulation threshold (Behnood-Rod et al., 2020). Thus, the ICSS results suggest lower brain rewarding effects of mitragynine as compared to morphine. Note that ICSS is not recommended in FDAs guidance for abuse potential assessment but is considered a potentially informative model (Henningfield, Comer, Banks, Coe, Collins, Cooper, Fantegrossi, Durgin, Heal, Huskinson, Lanier, Lynch, Miesch, Rowlett, Strickland, & Gannon, 2025). 2.2.3 Drug Discrimination Drug discrimination studies assess the interoceptive (subjective) effects of a substance by training animals to recognize and distinguish the effects of a test drug from a placebo (saline) or another drug. An animal's ability to generalize the subjective cue of a novel Page 12 of 128 compound to that of a known drug of abuse, such as morphine, is considered predictive of similar subjective effects and abuse potential in humans. Several studies have shown that 7-OH fully substitutes for the discriminative stimulus effects of morphine. Harun et al. (2015) trained male Sprague Dawley rats to discriminate morphine (5.0 mg/kg, intraperitoneal [i.p.]) from saline. In subsequent substitution tests, the highest dose of 7-OH (3.0 mg/kg) produced complete substitution for the morphine cue, and this effect was reversed by the opioid antagonist naloxone. Notably, this study found 7-OH to be more potent than morphine in producing these subjective effects. Further research has reinforced these findings. Obeng et al. (2021) reported that 7-OH fully generalized to morphine in rats, whereas mitragynine only partially generalized. Similarly, Hemby et al. (2019) found that 7-OH substituted for morphine in a dose- dependent manner, while mitragynine did not substitute at any dose tested. The consistent and complete generalization of 7-OH to the morphine cue across multiple studies provides strong evidence that it may produce subjective effects that are qualitatively similar to those of classical opioids. 2.2.4 Conditioned Place Preference Matsumoto et al. (2008) found that 7-OH administered at 2 mg/kg produced conditioned place preference (CPP) with greater potency than morphine. Similarly, Gutridge et al. (2020) demonstrated that 7-OH at a dose of 3 mg/kg induced CPP in C57BL/6 mice, although it required four conditioning sessions compared to 2 sessions for morphine (6 mg/kg) to establish the preference. This suggests that while 7-OH is rewarding, the onset or strength of the conditioned association may differ from that of morphine under certain experimental conditions. Another study by Chakraborty, Uprety, et al. (2021) also confirmed that 7-OH produces significant CPP, whereas its metabolite, mitragynine pseudoindoxyl, did not, indicating distinct rewarding profiles among related alkaloids. Collectively, these findings consistently show that 7-OH has rewarding effects sufficient to establish a conditioned preference, common in drugs with abuse potential. 2.3 Clinical Studies and Evidence of Abuse Potential in Humans While there have been no controlled human laboratory studies conducted to date specifically designed to assess the abuse potential of 7-OH, a growing body of epidemiological data, clinical case reports, and user self-reports provide evidence of its nonmedical use and abuse. The FDA's 2025 scientific assessment noted clinical presentations that include reports of “euphoria, sedation, respiratory depression, and opioid-like withdrawal syndromes, with users acknowledging its significant addiction potential”. These reports align with the effects predicted by preclinical models and are characteristic of substances with abuse potential, discussed further in Factors 4-6. 2.4 Implications for Abuse Potential Taken together, the evidence summarized in Factor 1 suggests that 7-OH has meaningful abuse potential despite limitations in the breadth of available studies, the range of study types, and inconsistencies across findings. Preclinical studies suggest robust reinforcing, rewarding, and subjective effects characteristic of a µ-opioid agonist, Page 13 of 128 with potentially a potency greater than morphine, although not necessarily stronger. This distinction is often misunderstood; potency refers to the amount of drug required to produce a given effect and not the maximal possible effect that can be produced. Thus, for example, in a classic study, Matsumoto et al. (2004) found that the potency of 7-OH varied widely across outcome measures (include guinea-pig ileum contractions, tail flick and hot plate tests) as compared to morphine and mitragynine, however, whereas 7-OH and morphine produced similar maximum effects on several measures, mitragynine’s effects were consistently weaker (producing smaller maximum possible effects) and far less potent (taking more mg to produce any effect) than 7-OH and morphine. From an abuse potential perspective, the most important finding is that both 7-OH and morphine produce a range of qualitatively similar effects, supporting the characterization of 7-OH as an ‘opioid’ and as a drug with a potential for opioid-like abuse potential. These findings are also consistent with similarities in receptor binding and mechanism of action, suggesting that its abuse related pharmacology is sufficiently similar to that of opioids to warrant considering characterizing of 7-OH as an opioid. At present, the available evidence does not provide a basis for determining the overall abuse potential of 7-OH relative to morphine. However, that level of pharmacological characterization is not critical to determine whether a substance lacking FDA approval or commonly accepted for medical use meets the requirements for placement into Schedule I of the Substances Act. That 7-OH as a substance exhibits meaningful abuse potential and overall morphine-like opioid pharmacology satisfies the statutory criteria for scheduling. If 7-OH were to be submitted to FDA as part of a New Drug Application and subsequently approved for therapeutic use, a quantitative determination of its relative abuse potential would be important to guide scheduling – for example if it should be placed alongside morphine in Schedule II, or in a less restrictive schedule (III, IV, or V) based on the totality of evidence. 3 Factor 2: Scientific Evidence of its Pharmacological Effects Current scientific evidence shows that 7-OH is pharmacologically active with a distinct profile of central nervous system (CNS) mediated effects. It acts primarily as a potent partial agonist at the MOR, but its effects extend to other neurotransmitter systems, indicating that while its effects appear to warrant the designation as an opioid, it has additional effects that appear to differentiate 7-OH from morphine-type opioids in its overall pharmacology. 3.1 Mechanism of Action and Opioid Binding 7-OH’s interactions with opioid receptors appear to be the predominate cause of at least its abuse related effects. For example, 7-OH consistently demonstrates high affinity for the MOR, with reported inhibitor constant (Ki) values ranging from approximately 7 nM to 78 nM, significantly higher than that of mitragynine, its parent alkaloid (1700 nM). Studies have shown that both 7-OH and mitragynine demonstrate a preference for activating the G-protein signaling pathway with little to no recruitment of the β-arrestin-2 pathway. This is a significant finding, as β-arrestin-2 recruitment is strongly associated Page 14 of 128 with the adverse effects of classical opioids, such as respiratory depression and constipation. This G-protein bias suggests a potential for a lower risk profile compared to conventional opioids like morphine, which robustly recruit β-arrestin-2 (Ellis et al., 2020; Kruegel et al., 2016). Nonetheless, other findings with 7-OH indicate meaningful opioid-like abuse potential, as discussed in Factor 2. For example, in addition to its primary action at the MOR, 7-OH also binds with moderate to high affinity at the kappa (κ-) opioid receptor (KOR) and DOR, where it appears to function as a competitive antagonist (Obeng et al., 2021). This profile as a partial MOR agonist and a KOR/DOR antagonist distinguishes it from classical opioids like morphine, which are full MOR agonists, and may contribute to its unique pharmacological effects. For instance, KOR antagonism is associated with antidepressant and anxiolytic effects, which could align with some of the reported motivations for kratom and 7-OH use (Carlezon, & Krystal, 2016). 3.2 Effects on Other Neurotransmitter Systems While 7-OH appears to primarily target opioid receptors, there is evidence that it, along with mitragynine, also interacts with other CNS receptors, including adrenergic, serotonergic, and dopaminergic systems. This multimodal activity likely contributes to the complex profile of effects reported by users, which can include both stimulant-like and sedative properties. A study by James P. Manus et al. (2025) investigated the effects of 7-OH on dopamine release in the nucleus accumbens, a key brain region in the reward pathway. The study found a bidirectional effect: a low dose of 7-OH (0.5 mg/kg) increased dopamine release, while a high dose (2 mg/kg) decreased it. The authors noted that these alterations in dopamine function are not necessarily consistent with those of classic drugs of abuse, suggesting a more complex mechanism of action on the brain's reward systems. Ellis et al. (2020) found that the oxidation of mitragynine to 7-OH significantly strengthens its binding affinity at the MOR but weakens its affinity at adrenergic and serotonin receptors, indicating that the pharmacological profile shifts substantially upon metabolism. 3.3 Antinociception Numerous studies have demonstrated that 7-OH produces robust, dose-dependent antinociceptive effects in animal models such as the hot plate and tail flick tests (Behnood-Rod et al., 2020; Matsumoto et al., 2004). Its potency in producing analgesia is consistently reported to be significantly greater than that of morphine. For example, Kruegel et al. (2016) reported that 7-OH was approximately 10 times more potent than morphine in producing antinociception. This potent analgesic effect, combined with its high oral bioavailability compared to morphine, and its lack of measurable β-arrestin-2 recruitment makes 7-OH an interesting subject for potential therapeutic development. 3.4 Respiratory Depression While studies referenced above determined mitragynine and 7-OH lacked measurable β-arrestin-2 recruitment, a study by Gonzalez et al. (2025) found that 7-OH caused dose-dependent reductions in respiratory frequency and minute volume in rats, effects Page 15 of 128 fully reversed by naloxone. This is in contrast to mitragynine, which unexpectedly increased respiratory frequency with no significant depression of tidal/minute volume. This lack of respiratory depressive effects by mitragynine was confirmed by Henningfield, Rodricks, et al. (2022)’s study showing no respiratory depression in rats administered up to 400 mg/kg oral mitragynine. Mitragynine’s stimulant effect was not blocked by naloxone, suggesting a non-opioid mechanism. 3.5 Comparison to Morphine Comparing the relative potency of kratom, mitragynine, and 7-OH to morphine is important in pharmacological evaluations but is often misinterpreted as indicative of abuse, addiction and/or harm potential. What is more important in abuse potential assessments is the maximum possible effect of a drug as a reward or euphoriant which is generally considered a stronger determinant of the overall abuse potential of a drug and its likelihood of recreational use. Potency should not be considered the same as maximum possible effect. Numerous studies have shown that 7-OH is more potent than morphine on several measures but most of these do not suggest that 7-OH has stronger maximum possible effects. For example, an in vitro study using electrically stimulated guinea pig ileum, a classic assay for opioid activity, found that 7-OH was approximately 17 times more potent than morphine and 30 times more potent than mitragynine (Horie et al., 2005). A similar study by Takayama et al. (2002) found that 7-OH had 13 times higher potency than morphine and 46 times more than mitragynine. Studies of 7-OH’s antinociception potential have reported it at 10 times that of morphine (Kruegel et al., 2016). However, it is critical to interpret these findings with caution. While informative, results from in-vitro assays and subsequent in-vivo animal models do not always directly translate to the complex human experience. Also, while 7-OH’s affinity to opioid receptors relative to morphine can be quantified in a controlled laboratory setting, their respective pharmacological profiles merit further study. Factors such as route of administration, formulation, metabolism rate, bioavailability, blood-blood brain barrier penetration, and the activation and interactions of multiple neurotransmitter systems create a more complex web of effects than can be observed in a controlled laboratory setting. Therefore, while the existing research provides a valuable pharmacological baseline establishing 7-OH as a potent opioid agonist in some assays, its overall pharmacological effects in humans have not been well characterized and remains an area requiring further clinical research. 3.6 Implications for Abuse Potential Taken together the data reviewed in this factor are consistent with the characterization of 7-OH as a CNS-acting drug with effects likely to contribute to use and abuse potential. Data from numerous studies indicate that 7-OH is pharmacologically active with dose-related effects and mechanisms of action being similar though not identical to those of morphine-like opioids. The relative potency compared to morphine appears to vary widely across measures, which is not surprising nor atypical of opioids. However, its distinct activity and variability (especially its lack of measurable β-arrestin-2 recruitment and activity at KOR and DOR receptors) suggest that direct comparison and Page 16 of 128 characterizing 7-OH as an opioid that is up to 13 times more potent than morphine is misleading as a stand-alone indicator of its abuse potential as these estimates are based on animal models that may not necessarily relate to human effects. Moreover, as mentioned earlier, relative potency is not necessarily indicative of abuse potential. The mixed mechanisms of action of 7-OH may contribute to the diversity of reasons people report for its use (as discussed in Factors 4, 5, and 6); however, this pharmacological complexity does not inherently determine its level of abuse potential. For example, when seeking rewarding and euphoriant effects, many recreational users prefer opioids with a pharmacological profile characterized predominantly by MOR agonism, such as morphine, oxycodone, heroin and fentanyl. Overall, the risk profile of 7-OH remains incompletely understood and warrants further study. 4 Factor 3: Current State of Scientific Knowledge Research on kratom, including research on 7-OH specifically, has increased enormously in the past decade. For example, the introduction to Kratom: History, Science, and Therapeutic Potential, a recently published book featuring contributions from many of the world’s leading kratom researchers, notes the rate of annual kratom science publications increased from about 20 per year in 2016 to more than 130 per year by 2024, with the increased fueled heavily by research funding by the National Institutes of Health (NIH), NIDA (Henningfield, Beyer, & Raffa, 2025). This rapidly expanding body of research undoubtedly played a significant role in shaping two important themes in the July 29, 2025 FDA and DHHS documents addressing 7-OH: the characterization of its abuse potential and safety, and the decision to treat 7-OH as a public health concern distinct from kratom itself. One of the most significant advances to emerge from the hundreds of new studies conducted over the past decade has been the understanding that 7-OH is more appropriately considered a mitragynine metabolite in humans and animals that are given or who self-administer kratom. Additionally, while it has been established that it is either absent from or appears in de minimis levels in freshly harvested kratom leaves, 7- OH may emerge at low levels in the leaves over time, likely as a result of enzymatic processes (Karunakaran, Vicknasingam, & Chawarski, 2025; Smith et al., 2024). Indeed, it was observed several decades ago that 7-OH is less than 2% of the total content of all of the alkaloids in kratom leaves (Takayama, 2004). In many marketed kratom products including leaf powder, encapsulated kratom powder and extracts in the U.S. 7-OH content is lower still ranging from undetectable to about 0.01% to 0.04% by weight (Kikura-Hanajiri et al., 2009). 4.1 Pharmacokinetics When kratom or pure, single isolate mitragynine extracts are self-administered or administered in clinical studies, mitragynine is metabolized in the liver, a conversion mediated primarily by the CYP3A enzyme, forming 7-OH. A human clinical study by Mongar et al. (2024) found that co-administration of itraconazole, a potent CYP3A4 inhibitor, decreased the formation of 7-OH from mitragynine, reducing its peak plasma concentration (i.e., Cmax) by 56% and its total exposure (i.e., area under the curve) by 43%. Page 17 of 128 A large scale clinical trial found that after administration of encapsulated kratom leaf powder, the time to reach maximum plasma concentration (i.e., Tmax) for 7-OH was between 1.2 and 2.0 hours (Huestis et al., 2024). The elimination half-life (i.e., T1/2) was found to be 4.7 hours after a single dose and extended to 24.7 hours after multiple daily doses, indicating potential for accumulation with long term and/or daily use. A study in beagles found a conversion rate of 23.1% of mitragynine to 7-OH, though this may not be representative of human conversion rates. For instance, Hiranita et al. (2020) reported “the conversion rate of 7‐hydroxymitragynine from per oral (PO) mitragynine is low. In a study of pharmacokinetic interaction of kratom and cannabidiol in male rats, the metabolite to parent (mitragynine) exposure ratio percentage of 7-OH- MG remained similar (3.5 and 3.1 with and without cannabidiol, respectively). As there was an increase in mitragynine exposure during this study, it was expected that this would be due to a decrease in metabolism, but this was not the case for 7-OH-MG despite it being primarily metabolized by CYP3A and cannabidiol being a competitive inhibitor of CYP3A (Berthold et al., 2024). Further rat studies support this finding, showing that 7-OH and mitragynine are quantifiable 8 hours after consumption, and accumulation of mitragynine and 7-OH after multiple oral doses (Chiang et al., 2024; Kamble et al., 2021). Another study by Tanna et al. (2022) reported a similar half-life of 5.67 hours after a single oral 2 g dose of kratom tea. This tea was tested and found to have contained only trace amounts of 7- OH (i.e., less than the limit of quantitation [< LOQ]) in the starting product; therefore, the assumption was made that 7-OH was generated from the metabolism of mitragynine in vivo. Concerningly, there appear to be some 7-OH formulations that have been designed to bypass first pass metabolism, artificially increasing bioavailability (Smith et al., 2025). Kruegel et al. (2019) found that brain concentrations of 7-OH formed from mitragynine in mice are sufficient to explain most or all of the opioid-receptor-mediated analgesic activity of mitragynine. At the same time, mitragynine is found in the brains of mice at very high concentrations relative to its opioid receptor binding affinity, suggesting that it does not directly activate opioid receptors (Kruegel et al., 2019). Uchaipichat (2025) found that 7-OH-MG exhibited inhibitory potency on UGT1A9, with a half-maximal inhibitory concentration (IC50) value of 51 µM, while moderate potency was observed for UGT1A1 and UGT1A3, with IC50 values of 196 and 141 µM, suggesting the potential for herb-drug interactions in individuals consuming high doses of 7-OH- MG. However, the experimental Ki values found in this study were relatively high compared to the maximum plasma concentrations of mitragynine and 7-OH reported in humans. In a study relevant to breast cancer treatment medications are potential effects of 7-OH (and mitragynine) on as HER2 inhibitors. This in silico study (involving computer simulations to predict pharmacological effects) suggested that the molecular docking included binding energies of −7.56 kcal/mol and −8.77 kcal/mol, respectively, with key interactions involving residues such as Leu726, Val734, Ala751, Lys753, Thr798, and Page 18 of 128 Asp863. Akbar et al. (2025) found both mitragynine and 7-OH were inhibitors of CYP2D6 and CYP3A4, though neither were found to be P-glycoprotein substrates, which minimizes the risk of efflux-related bioavailability issues. Both studies confirm the potential for significant drug-drug interactions with other substances that are substrates, inhibitors, or inducers of these systems. These should be considered preliminary findings and not necessarily related to abuse potential or safety but provide an example of other research that involves 7-OH and other mitragynine related substances. While Akbar et al. (2025)’s Absorption, Distribution, Metabolism, Excretion, and Toxicity analysis found that both mitragynine and 7-OH demonstrated high gastrointestinal (GI) absorption, suggesting high oral bioavailability (also a conclusion by Chakraborty, Uprety, et al. (2021), a study in rats reported a low oral bioavailability of only 2.7%, possibly due to poor water solubility, indicating that formulation and species differences may significantly impact absorption (Chiang et al., 2025). A recent case report that has been accepted for publication at the time of this writing described a patient admitted to a hospital emergency department following "cardio- pulmonary arrest”. He was found unresponsive and received approximately 10 min of cardiopulmonary resuscitation; he was successfully revived with two doses of naloxone 4mg intravenously." The patient reported ongoing use of other substances that may have contributed to this event, as well having ingested several times the recommended serving size labeled on the 7-OH product. Thus, whereas causality cannot be definitively determined beyond a likely poly-pharmaceutical contribution is not clear, the responsiveness to naloxone suggests that 7-OH’s opioid receptor-mediated activity may have played a role, particularly since no other conventionally screened 'opiates' were detected in the blood (Pullman, Kanumuri, Leon et al. 2025). 4.2 Mitragynine Pseudoindoxyl Kamble et al. (2020) further discovered that 7-OH is itself converted to mitragynine pseudoindoxyl in human plasma, and to a greater extent than is produced in mice, rats, dogs, and cynomolgus monkeys, possibly explaining potential human effects that may not be predicted in animal studies alone. Mitragynine pseudoindoxyl’s effects, however, are still mostly unclear; for instance while 7-OH-MG and mitragynine have shown significant conditioned place preference (Section 2.2.4), mitragynine pseudoindoxyl did not (Chakraborty, DiBerto, et al., 2021). 4.3 Conclusions The available evidence shows that 7-OH is a potent, orally bioavailable, µ-opioid partial agonist with a G-protein bias that can accumulate in the body upon daily and/or chronic use. Its metabolism is heavily dependent on the CYP3A4 enzyme processes. Its complex pharmacology, involving interactions with multiple opioid receptor subtypes and other neurotransmitter systems, underlies its opioid-like effects, including analgesia, euphoria, and sedation, as well as its potential for abuse and dependence. Page 19 of 128 5 Factors 4, 5, and 6: History and Current Patterns of Abuse; The Scope, Significance and Duration of Abuse; What, if any, Risk is there to the Public Health 5.1 Factor 4: History and Current Patterns of Abuse The marketing and apparent sales and consumption of 7-OH have increased rapidly since about 2022, and 7-OH has progressed over the past several years from a minor, little known alkaloid with little to no independent history of use to a commercially available, highly concentrated product at the center of what FDA deems an “emerging public health threat”. This has been driven in part by growing awareness of its potentially potent opioid pharmacology though current use patterns (as gleaned from national surveys, surveillance systems, and online user communities) reveal a user base with diverse motivations. However, these data sources also highlight an escalating pattern of high-dose use of concentrated products that is associated with dependence, withdrawal, and other adverse outcomes. Traditional use of kratom in Southeast Asia, which involves chewing fresh leaves or brewing them into tea, results in ingestion of only trace amounts of 7-OH. The primary psychoactive effects from traditional kratom preparations are attributed primarily to its most abundant alkaloid mitragynine and the complex interactions of the many other alkaloids in the plant leaves. The market for kratom began to rapidly evolve with the rise of its popularity in the U.S. in the mid-2000s, though use likely dates back as early as the 1980s, brought back by American veterans returning from Southeast Asia and immigrants from those areas. Consumer demand for alternative kratom products, combined with scientific and manufacturing resources and innovation from American entrepreneurs led to explosive growth in the number of kratom extracts and other products artificially enhanced with non-natural amounts of kratom alkaloids and/or other substances. A pivotal shift occurred with the proliferation of products specifically marketed as “7-OH” products. These products often contain artificially elevated levels of 7-OH, often created through synthetic or semi-synthetic means, such as chemical oxidation of mitragynine, which is much more readily abundant naturally and economically viable than isolating from kratom leaves. Analysis of these commercial products revealed concentrations of 7-OH that are hundreds of times higher than would be expected in natural kratom leaf. For example, one analysis reported that 7 of 8 products tested contained 109-509% more 7-OH than would be expected in a natural product (Ogozalek, 2023), and news reports identified pill products containing 15 mg of 7-OH per pill, a dose far exceeding natural levels and one that is likely pharmacologically significant. This is in contrast to an analysis of 13 commercial kratom products, which found 7-OH at 0.01-0.04% by weight, aligning with reports that 7-OH represents less than 0.05% of the alkaloid content, substantially lower than mitragynine. This indicates that naturally occurring levels of 7-OH in kratom are minimal compared to the primary alkaloid (Kikura-Hanajiri et al., 2009; Kruegel et al., 2019). These 7-OH products are now readily available online and in retail locations such as gas stations, vape shops, convenience stores, and corner shops, often in a vast Page 20 of 128 array of formulations like gummies, tablets, and liquid shots (Hill, Henderson, et al., 2025). 5.1.1 Reasons for Use While national surveys like the National Survey on Drug Use and Health (NSDUH) track kratom use, they do not yet specifically distinguish users of traditional kratom from users of concentrated 7-OH products. General kratom user demographics from the 2019 NSDUH and other surveys indicate that users are generally somewhat more male than female users, with most identifying as “White” or Caucasian, and between the ages of 18 and 49, though results vary widely. The most recent largescale kratom survey at this writing reported the majority of kratom users were males between 30-49 years old who identify as Caucasian (Grundmann et al., 2025). There is evidence that kratom users are generally older, often reporting reasons for use related to potential therapeutic effects (relief of common pain symptoms, elevating energy); there is little evidence of youth use. However, none of these surveys addressed people who are primarily 7-OH consumers, a critical area in need of research. Thus, extrapolations from kratom-focused surveys are not necessarily representative. This caveat applies to reasons for use as well, although some anecdotal data described below suggest that at least some 7-OH users are people who found it to be more effective or satisfying than kratom for pain and self- management of their opioid use disorder and/or opioid withdrawal. Those who use kratom and 7-OH report a diverse range of motivations, including for therapeutic or self-medication purposes, such as for pain relief, anxiety, and depression. A significant portion of users, particularly those with a history of opioid use, report using kratom to address opioid withdrawal symptoms or as a substitute for more dangerous illicit opioids. Additionally, current opioid users were more likely to report use kratom for opioid withdrawal, while former opioid users were more likely to report mood elevation as their reason for use (Singh et al., 2020). The emergence of concentrated 7-OH products appears to be attracting both existing kratom users and new consumers. Analysis of Reddit discussions reveals two primary user groups for 7-OH: individuals seeking potent relief for chronic pain, and individuals seeking strong, opioid-like recreational effects. For example, one Reddit user in a chronic pain forum reported using 7-OH for pain management, often at lower daily doses (e.g., 11 mg/day) without reporting significant adverse effects. In contrast, discussions in subreddits focused on substance use and quitting kratom describe patterns of high-dose, frequent use for euphoric effects, leading to rapid development of dependence and severe withdrawal. This bifurcation suggests that the availability of a more potent, isolated compound is creating distinct patterns of use and risk profiles compared to traditional kratom. 5.1.2 Dosing, Routes of Administration, and Trajectory of Use Information from online user reports provides detailed, albeit anecdotal, data on current use patterns for 7-OH products. An analysis of 6 Erowid experience reports found a median oral dose of 13.5 mg (range 6.9 mg - 16.9 mg), with a maximum reported dose Page 21 of 128 of 120 mg. Most reports described oral administration of pills, capsules, or tablets, though sublingual and insufflation (snorting) routes were also mentioned. A concerning pattern emerging from these reports is the trajectory of use. While some reports describe single-dose experiences, a significant portion describe daily use, escalating over periods from a few days to several months. Reddit users in the “Quitting Kratom” subreddit describe daily use, sometimes up to 5× per day, with doses associated with withdrawal symptoms ranging from 30 mg/day to as high as 500 mg/day. This pattern of escalating, high-frequency dosing is a classic hallmark of substance use disorders and is consistent with the development of tolerance to 7-OH's effects. The availability of 7-OH in discrete, high-dose units like pills and liquid shots facilitates this pattern of use in a way that traditional kratom use (i.e., consuming dried kratom leaf powder) does not. 5.2 Factor 5: Scope, Duration, and Significance of Abuse National surveillance systems in the U.S. have in recent years begun tracking use of kratom; however, the majority of these systems have yet to track data as it relates to 7- OH use, and attempts at analysis with current data are complicated by these systems combining 7-OH and kratom cases as one category. However, recent efforts to monitor 7-OH specifically, combined with analyses of existing data, reveal concerning signals of increasing human exposure and associated risk as discussed by FDA (Reissig et al. 2025) and in this Factor. The scope of use appears to be significant and growing, marked by a sharp increase in incidents beginning in late 2023 and continuing through 2025. Adding to the domestic data, the UNODC has noted that since 2024, the U.S. and other jurisdictions worldwide have reported toxicology cases involving high-concentration 7- OH products to its Early Warning Advisory on New Psychoactive Substances (UNODC, 2025). See further discussion relevant to scope and significance in Factors 4 and 6. 5.2.1 National Surveillance Systems 5.2.1.1 FAERS FAERS reports involving 7-OH were identified through searches of the FAERS Public Dashboard and open FDA using the term “7-Hydroxymitragynine,” limited to cases in which 7-OH was designated as the primary suspect drug. No date restrictions or deduplication procedures were applied. The two sources largely overlapped, though 2 cases appeared exclusively in the Public Dashboard. In total, 14 unique cases were identified. Corresponding data were extracted from open FDA and qualitatively reviewed. A summary of findings is presented below. The 14 FAERS case reports involving 7-OH primarily describe patterns of dependence, withdrawal, and psychiatric disturbances. Across patients ranging from their early 20s to mid-60s, reactions commonly included drug dependence, withdrawal syndrome, depression, anxiety, insomnia, somnolence, and impaired quality of life. Several cases noted GI complaints (e.g., nausea, vomiting, diarrhea, constipation), neurological issues Page 22 of 128 (e.g., dyskinesia, memory problems, dizziness), or musculoskeletal symptoms (e.g., myalgia, restless legs). Some patients reported product quality concerns or suspected tampering, suggesting variability in supply or formulation. Many cases involved concomitant use of prescription medications (e.g., clonidine, gabapentin, antidepressants, Suboxone, benzodiazepines) or other herbal mitragynine products, complicating causality assessments. Importantly, 2 fatal cases associated with 7-OH consumption were recorded: one involving toxicity from multiple agents including opioids and mitragynine in a 38-year-old male, and another describing accidental poisoning and respiratory depression in association with polypharmacy (including citalopram, lamotrigine, and zopiclone) in a male from Norway. These highlight potential risks of combining 7-OH with other CNS- active substances. Overall, the data remain sparse but suggest that 7-OH is more frequently linked to dependence, withdrawal, psychiatric symptoms, and – in rare but severe cases – fatal outcomes, warranting continued monitoring and further investigation. 5.2.1.2 National Poison Data System Between February 1, 2025 and April 30, 2025, the National Poison Data System (NPDS) recorded 53 closed human exposure cases involving 7-OH (Table 1). Of these, 24 were classified as abuse cases, and 37 involved single-substance exposures, including 16 single-substance abuse cases. The most common reasons for exposure were intentional abuse (24 cases, 16 single-substance), withdrawal-related use (8 cases, 6 single-substance), and unintentional general exposure (4 cases, all single- substance). Smaller numbers were attributed to suspected suicide (2 cases), adverse drug reactions (4 cases), misuse (3 total cases), therapeutic error (4 cases), and unknown reasons (2 cases). Most reported clinical effects were moderate (13 cases, 6 single-substance) or minor (6 cases, 3 single-substance), with 3 major outcomes (including 1 single-substance). Five cases were judged as having minimal effects, and one was considered a potentially toxic exposure but could not be followed. Age distribution showed that the majority of cases occurred in adults (≥18 years; 46 cases, including 23 abuse cases and 32 single-substance exposures), while 6 cases involved individuals under 18, and 1 case had unknown age. Table 1. National Poison Data System Closed Human Exposure Casesa (01Feb2025-30Apr2025) Number of Exposure Casesb Number of Abuse Casesc Single Substance Exposure Cases Single Substance Abuse Cases Total cases involving 7-OH 53 24 37 16 Reason Page 23 of 128 Number of Exposure Casesb Number of Abuse Casesc Single Substance Exposure Cases Single Substance Abuse Cases Adverse drug reaction 4 2 Intentional- abuse 24 16 Intentional- misuse 4 3 Intentional- suspected suicide 2 0 Other- withdrawal 8 6 Unintentional- general 4 4 Unintentional- misuse 1 1 Unintentional therapeutic error 4 3 Unknown reason 2 2 Related Clinical Outcomes Minor 6 3 Moderate 13 6 Major 3 1 Note followed, minimal clinical effects possible 5 3 Unable to follow, judged as potentially toxic exposure 1 0 Age < 18 years 6 1 5 0 ≤ 18 years 46 23 32 16 Unknown age 1 0 0 0 Abbreviations: 7-OH = 7-hydroxymitragynine; NPDS = National Poison Data System. Note: Related clinical outcomes includes cases with clinical effects deemed “related” to exposure based on timing, severity, and assessment of clinical effects by Poison Center Specialists. Definitions available from America’s Poison Centers: NPDS Full Report 2023 (Gummin et al., 2024, p. 235). a Excludes cases classified as ‘confirmed non-exposure’. b Cases may involve other substances, besides 7-OH. Source: Adapted from NPDS dataset. 5.2.1.3 National Forensic Laboratory Information System (NFLIS) The National Forensic Laboratory Information System (NFLIS) collects drug identification results obtained during law enforcement investigations involving potential Page 24 of 128 criminal possession and distribution of illicit drugs and substance seizures collected during those operations. Historically, mitragynine has never reached the threshold to be listed among the top 25 most frequently identified drugs, though it has appeared in lower-level reports. Mitragynine has not been reported in annual NFLIS reports because its levels have been relatively stable and low since about 2015. However, data can be obtained from the NFLIS Public Data Query System. As of August 2025, data from the NFLIS Public Data Query System showed 253 mitragynine drug reports in 2024, but specific data for 7-OH seizures are not yet separately reported in publicly available annual summaries. The lack of 7-OH specific data in law enforcement seizure reports represents an important current gap in surveillance. 5.2.1.4 DEA Toxicology Testing Program (DEA TOX) The DEA TOX program analyzes toxicological evidence from death investigations. Between 2019 and 2025, 103 cases were identified where mitragynine, 7-OH, or mitragynine pseudoindoxyl were detected. A significant limitation of this data is the difficulty in discerning whether deaths are related to one specific alkaloid, as 7-OH is a metabolite of mitragynine. However, the report notes a trend: the number of fatal overdose cases in which one or more of these substances were detected was approximately 3-fold higher for the years 2023 to 2025 compared to the period from 2019 through 2022. This increase coincides directly with the recent market entry of concentrated 7-OH products, suggesting a strong temporal association between the availability of these new products and fatal outcomes. It is important to note that many reported kratom-associated deaths involve toxic levels of other substances, and many lack the comprehensive toxicological testing needed to confirm a causal role for either mitragynine or 7-OH. Kratom products may also be present at opioid-related fatalities because they are often used to manage opioid use disorder or withdrawal. Additionally, routine toxicology screens may miss novel psychoactive substances, such as designer opioids or benzodiazepines, requiring more specialized and costly testing (Henningfield, Grundmann, Huestis, and Smith, 2024) 5.2.1.5 Other National Surveillance Data Two important national surveillance systems that monitor substance use trends, NSDUH and the proprietary Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS) (which also receives federal funding), have included “kratom” as a tracked substance” but have not differentiated traditional kratom products from concentrated 7-OH products. NSDUH provides prevalence estimates for kratom use (0.6% past-year use in 2024) but does not yet differentiate 7-OH use. As a result, their reported “kratom” data likely represent a combined population of kratom users and those using 7-OH products, a segment that appears to have emerged and grown rapidly in recent years. A further challenge in these surveillance efforts is that some individuals who use 7-OH may continue to report their past or current use simply as “kratom”, even when the product in question would more accurately be classified as a 7-OH product. These two surveillance systems also likely underestimate kratom use overall, possibly due to their survey designs and sampling approaches that primarily target major illicit and prescription drug use (see discussion in Henningfield, Grundmann, et al. (2022). These Kratom focused reports suggested estimates of approximately 1.7 to 2.0 million Page 25 of 128 past-year kratom consumers from 2019–2021 (Palamar, 2021; SAMHSA, 2023, 2024), with an estimated lifetime prevalence at 3.4 million based on 2018–2019 data (Schimmel, & Dart, 2020). Other major surveillance systems, such as the Drug Abuse Warning Network (DAWN), which tracks drug-related emergency department visits, and the Treatment Episodes Data Set (TEDS), have not yet reported specific data for 7-OH, though the “New DAWN” system recently identified “7-OH” as a new slang term to monitor. A more recent nationally representative survey suggests past 30 day (‘current use’) prevalence suggests potentially more than 20 million kratom users ages 18 and older (Grundmann et al., 2025).The recency of this survey conducted in 2024 makes it likely that some respondents were actually primary 7-OH users, possibly contributing to the larger estimated population of kratom consumption in earlier surveys. Similarly, it is possible if not plausible that some fraction of adverse events reported to FDA’s Adverse Event Reporting System, to the poison control centers, and possibly deaths associated with kratom consumption involved consumption of 7-OH products in addition to or in place of kratom products that do not contain artificially boosted or high concentrations of 7-OH. This conclusion is consistent with the following observations by FDA in its Reissig-led scientific evaluation (Reissig et al., 2025): “Available surveillance data indicate that abuse of 7-OH is occurring and is associated with serious harms; however, as noted previously, it is difficult to quantify the public health burden because surveillance systems do not provide estimates for the prevalence of 7-OH use and are only beginning to track the specific involvement of 7-OH enhanced products in exposure cases and overdoses. The current epidemiologic data on 7-OH exposures often lack sufficient detail to distinguish with confidence involvement of botanical kratom products from 7-OH enhanced products.” (Reissig et al., 2025, p. 14) And in its Conclusions section: “Due to the fact that 7-OH is both a metabolite of mitragynine and naturally present in low amounts in botanical kratom, using toxicology results to identify 7- OH as a primary or sole contributor in human exposures is challenging. There is also a need for improved clinical awareness and population surveillance to better characterize patterns of 7-OH use, the products that people are obtaining, and individual treatment needs following 7-OH exposure. Additionally, questions on 7- OH are not generally included in national surveys, and other data sources that rely on self-reported use of 7-OH likely underestimate the number of 7-OH exposure cases, as individuals may be unaware of the distinction from kratom products. Nonetheless, since specific codes were added earlier this year to document 7-OH exposure cases, U.S. poison centers have identified multiple single-substance cases of 7-OH exposure resulting in serious adverse clinical outcomes.” (Reissig et al., 2025, p. 18) Page 26 of 128 The foregoing observations of this report and those of Reissig et al. above are consistent with recent conclusions and evaluations by other experts which suggest that some fraction of the adverse events and possibly deaths that have been reported and or interpreted as involving or even caused by kratom, were actually more likely attributable to the consumption of 7-OH products in addition to or in place of kratom (Grundmann et al., 2024; Hill, Boyer, et al., 2025; Papsun et al., 2023; Smith et al., 2025; Vadiei, Evoy, & Grundmann, 2025). Taken together, the foregoing observations support the conclusion that it is urgent to add 7-OH to relevant substance surveillance systems including NSDUH, RADARS, FAERS, and poison control. Similarly, assessment of 7-OH in blood plasma in forensic toxicology examinations as well as kratom research in general is a critical need. It is beyond the scope of this report to specify how surveillance systems should be designed to distinguish between kratom products and those containing 7-OH, including the precise wording of survey questions or the analytical methods to detect 7-OH. These should be developed with input from appropriate experts and stakeholders, ideally with a fast-track approach with a proposal from FDA and request for comments. A public meeting for comment convened by FDA, ideally with NIDA and DEA involvement may also help to ensure that the approaches to surveillance and biological assessment will be scientifically reliable, valid, and relevant to the emerging marketplace, regardless of whether or not 7-OH is ultimately scheduled. 5.2.2 Published Case Reports Published case reports provide clinical evidence recorded and reported by trained healthcare professionals; however, these accounts are considered anecdotal and may not be representative of common experiences. A case report by Wightman and Hu (2025) detailed the experience of a 38-year-old man with a history of opioid use disorder who escalated his use from kratom to concentrated 7-OH products, consuming up to eight 30 mg tablets daily. Upon stopping, he experienced a clear opioid withdrawal syndrome, with a peak Clinical Opiate Withdrawal Scale (i.e., COWS) score of 14. His symptoms, which included anxiety, insomnia, and restlessness, were successfully managed with buprenorphine during an inpatient stay. Another case report described a 31-year-old who suffered severe substance-induced psychosis involving both kratom and cannabis, which resulted in self-amputation of his ears and penis (Broul et al., 2025). 5.2.3 Social Media Discussion To investigate online sources of discussion around 7-OH, the search terms “7-OH”, “7- OH-MG”, “7-OH-MIT”, and “7-Hydroxymitragynine” were included in a boolean search of Erowid (erowid.org) using the Google search term “7-OH OR 7-OH-MG OR 7-OH-MIT OR 7-Hydroxymitragynine site:erowid.org”, and of Reddit (reddit.com) using the Google search term “7-OH OR 7-OH-MG OR 7-OH-MIT OR 7-Hydroxymitragynine site:reddit.com”. The searches were completed in August 2025. Page 27 of 128 Six experience reports in the Erowid vault were found. Where provided, information on sex, age, body mass index, dose, route of administration, formulation, duration, and effects were recorded. Most (3/5 experience reports with dates) were recent (i.e., since 2024). The remaining 2 experience reports with dates described experiences from more than a decade ago (2007-2010). One experience report did not report its date. In terms of demographics, all 6 reports came from males aged 22 years to 39 years (i.e., younger adults). Across these 6 experiences, the median dose was 13.5 mg (interquartile range [IQR]: 6.9 mg – 16.9 mg) or 0.15 mg/kg body mass (IQR: 0.09 mg/kg – 0.19 mg). The maximum dose was 120 mg or 1.5 mg/kg. Two reports (33%) described single-dose experiences, 2 reports (33%) described daily use for 2 days, and 2 reports (33%) described longer-term, daily use from 2 weeks to 6 months. The majority (67% of reports) described oral administration of 7-OH, while the remaining reports described sublingual administration (n=1; 17%) and insufflation (n=1; 17%). The majority (67% of reports) described pill/capsule/tablet formulations, while the remaining 2 (33%) described tincture/liquid formulations. Experiences lasted from 3-6 hours. Only one report described concomitant substances, namely cannabis (smoked), though this does not necessarily mean that no other substances were taken. Effects included euphoria (83% of reports), cravings (50%), increased heart rate (33%), itch (33%), tiredness, lethargy, or sedation (33%), constipation (17%), self-reported “withdrawal” (17%), body shakes (17%), numbness (17%), weightlessness (17%), sick feeling (17%), feeling of relaxation (17%), aphrodisia (17%), analgesia (17%), loss of balance (17%), visual distortion (17%), and most significantly, hospitalization (17%) and self-reported “respiratory depression” (17%). The following review of Reddit posts and comments on 7-OH is non-exhaustive. On Reddit, 7-OH was discussed in the Quitting Kratom subreddit (www.reddit.com/r/quittingkratom). Reddit posts and comments were much less descriptive than Erowid experience reports making inferences difficult. Nevertheless, a number of Reddit users reported using or formerly using kratom and being offered 7- OH, sometimes for free, from stores where they would typically purchase kratom. Most users who reported 7-OH use reported pill/capsule/tablet forms; tinctures/liquid formulations were relatively rare. Most posts reported daily use, up to 5 × daily, with use duration from 5 days to 8 months. Some users attempted to dissuade others from 7-OH use. Effects were consistent with Erowid experience reports, including euphoria, withdrawal, anxiety, insomnia, restlessness, involuntary arm and leg movement, abdominal pain, vomiting, body shakes, tightness in chest, tachycardia, diarrhoea, fatigue, sedation, dizziness, paranoia, anhedonia, kidney pain, and 1 case of hospitalization. Some Reddit users compared the severity of withdrawal from 7-OH to other substances; these included “worse than how I was with the oxy withdrawal” and “50% as bad as Fentanyl withdrawal”. Some Reddit users described stopping 7-OH use “cold turkey”, or using kratom or other substances including suboxone to “taper off” of 7- OH. Many posts and comments were missing data on dose. Among comments reporting withdrawal symptoms and dose, these ranged from 30 mg/day to 500 mg/day. Many posts and comments were missing data on dose. Among comments reporting withdrawal symptoms and dose, these ranged from 30 mg/day to 500 mg/day. Many Page 28 of 128 posts and comments were missing data on dose. Among comments reporting withdrawal symptoms and dose, these ranged from 30 mg/day to 500 mg/day. 7-OH was also discussed by a number of Reddit users in the Chronic Pain subreddit (https://www.reddit.com/r/ChronicPain) who reported using 7-OH for chronic pain management. Only one Reddit user discussing 7-OH for chronic pain reported dose; they reported taking 5.5 mg tablets twice daily (11 mg/day) and did not report adverse effects or withdrawal or withdrawal. This is lower than the doses reported by Reddit users experiencing withdrawal. To quantify interest in 7-OH over time, Google Trends was used. Google search interest (i.e., the relative volume of Google searches) for “7-OH”, “7-OH-MG”, “7-OH-MIT”, and “7-Hydroxymitragynine” was extracted (Figure 1). Search interest in these search terms was zero from 2004 through 2010. Beginning in 2011, minimal search interest in “7-OH” and “7-Hydroxymitragynine” began, staying low through the end of 2023. Beginning in 2024 however, search interest in “7-OH” and “7-Hydroxymitragynine” grew rapidly, peaking in August 2025 shortly after FDA announced action on 7-OH products, which are the latest available data; search interest may continue to rise in the months following August 2025. Search interest in “7-OH-MIT” and “7-OH-MG” remained negligibly low throughout. Page 29 of 128 Figure 1. Google Search Interest in 7-OH-Related Search Terms Note: 7-OH-mitragynine may be referred to by the short-hand versions “7-OH”, “7-OH-MIT”, or “7-OH-MG”. Page 30 of 128 There are many websites that focus specifically on drug misuse and abuse, some intended to discourage such use as well as those that appear dedicated to providing information in support of, if not to encourage, misuse and abuse of drugs. Many of the kratom-related postings involve what appear to be extremely high dosages of kratom substances and extracts, and self-made extracts from a variety of kratom sources. For example, users may combine several grams of kratom powder, several ounces of kratom leaves, and indeterminate forms of this or other substances. Some people have reported experiencing intoxication, euphoria, and other effects at these very high dosages, though typically their comparisons to other drugs provide a basis for understanding why kratom and kratom products apparently are rarely the substance of choice among people who seek abused drugs and are in search of better ways to get better highs and euphoria. There are self-reports of dependence and withdrawal, but these tended to involve extremely high intakes of kratom, apparently along with other substances. 5.3 Factor 6: What, if any, Risk is there to the Public Health Factor 6 requires an integrated assessment of the overall risk a substance poses to public health. This involves synthesizing the pharmacological data on its intrinsic pharmacological risks (Factor 2), its potential for abuse and dependence (Factors 1 and 7), and the real-world evidence of its harm (Factors 4 and 5). For 7-OH, the available data indicate a potential risk to public health, which has led the FDA to conclude that it is a “dangerous substance” that poses an “emerging public health threat” and an “imminent hazard”. This risk is fundamentally driven by the substance's potent opioid pharmacology, exacerbated by its increasing availability in highly concentrated, unregulated products. Evaluation of Factor 6 can include individual and public health benefits evidence as well because real and perceived benefits can contribute to evaluating FDA approved pharmaceuticals as well as substances that have not been approved for therapeutic use (Henningfield, Coe, et al., 2022; Henningfield et al., 2025). FDA’s July 29, 2025 summary of the science (Reissig et al., 2025) and other FDA documents release on July 29 made clear the concerns of FDA and the DHHS have about the risks of 7-OH. In FDA’s July 29, 2025 educational slide set “Preventing the Next Wave of the Opioid Epidemic: What You Need to Know about 7-OH (FDA, 2025b), the second slide depicted four waves of the opioid crisis of approximately equal size and shape. These were labeled “prescription pills”, “heroin”, “fentanyl”, and “7-OH’, respectively. While the conclusion that 7-OH presents a potential and imminent public health risk necessitating regulatory attention is supported, caution is warranted against overstating the overdose risk, particularly given the likelihood of misinterpretation by the public and media when hearing references to 7-OH as “more potent than morphine”, even though the term “overdose” is not used in the figure. Despite evidence suggesting thousands of individuals are currently using 7-OH – including some who appear to be consuming highly concentrated preparations and substantial total doses – the documented incidence of fatalities directly attributable to 7- OH remains very low. Even if, as FDA has suggested, 7-OH-related deaths are Page 31 of 128 underreported, it is notable that such cases appear to be rare. This low apparent lethality may be explained by two key factors: first, the predominant route of administration among users is oral rather than intravenous; and second, 7-OH exhibits the pharmacological profile of a partial MOR agonist by several measures, as discussed in Factor 2. The available evidence indicates that 7-OH may indeed pose a “risk to public health” or a “national drug threat”, thereby warranting regulatory attention and interventions as discussed in Factors 4 and 5 and below. However, it remains uncertain whether 7-OH poses a population-level overdose risk comparable to that of other opioids. This uncertainty does not diminish the case for control measures; this report concurs that such measures – including potential scheduling under the CSA – are justified. However, it is important to recognize that some individuals report using 7-OH as their preferred and/or most effective alternative to opioids known to carry high risks of fatal overdose, or as a means of self-managing other serious disorders. Considering this population should inform any policy approaches, particularly those involving criminal penalties for possession if 7-OH is placed in Schedule I, as discussed in the policy section of this report. 5.3.1 Pharmacological Risks The primary risk inherent to 7-OH is its potent activity at the MOR, which mediates not only its abuse-related effects but also its most dangerous potential adverse effect: respiratory depression. As reported by Gonzalez et al. (2025), 7-OH produces dose- dependent respiratory depression that is reversible with naloxone, a classic feature of opioid toxicity. While some research suggests its G-protein bias and lack of measurable β-arrestin-2 recruitment may confer a degree of safety relative to classical opioids at equianalgesic doses, this risk may preclude 7-OH to be marketed as a dietary ingredient to be used in supplements regardless of whether it is placed in Schedule I. 5.3.2 Abuse, Dependence, and Withdrawal Risk While the abuse-related risk of 7-OH is primarily attributed to its effects at the MOR receptors, its pharmacology is not identical to that of classical opioids that are primarily active at the MOR (Factor 2). The FDA's 2025 assessment states that 7-OH produces “physical dependence, and withdrawal symptoms characteristic of classical opioids” and notes that clinical presentations include “opioid-like withdrawal syndromes” (Reissig et al., 2025). This is supported by published case reports in the medical literature, with reports of symptoms associated with opioid withdrawal including anxiety, insomnia, rhinorrhea, abdominal discomfort, restlessness, diaphoresis, and chills that were successfully managed with buprenorphine, a standard treatment for opioid withdrawal and dependence (Wightman, & Hu, 2025). However, these preliminary findings merit further study. As evidenced by user reports, the availability of potent products with concentrations of 7-OH that is far higher than is found naturally may be facilitating patterns of chronic, escalating dose use that can lead to dependence, withdrawal, and other symptoms associated with drugs of abuse. The consequences of this include not only the direct Page 32 of 128 risk of harm from the substance itself but also the broader medical, psychological, and social harms associated with addiction. The opioid-like withdrawal syndromes associated with 7-OH dependence presents another risk. Individuals attempting cessation may experience physical and psychological symptoms, which can be detrimental to their work and personal lives, a major barrier to recovery, and a cause to relapse. In some cases, individuals may require medically supervised withdrawal and medication-assisted treatment (e.g., with buprenorphine), placing additional burden on the healthcare system. 5.3.3 Potential Benefits to Consumers and Public Health Anecdotal reports in public media and other sources indicate that some 7-OH users perceive it to be more effective, acceptable, or accessible than FDA approved medicines, kratom, or other approaches for their conditions. Similar conclusions for kratom were reached in 2016 (Henningfield and Fant, 2016), and in subsequent analyses (Giroir, 2018; UNODC, 2021). Consequently, removal of 7-OH from the licit marketplace without simultaneously ensuring the availability of viable accessible alternatives carries the risks of unintended consequences. These include the risk that current 7-OH consumers may relapse to potentially deadlier opioid use, as well as the likely emergence of an illicit market in which 7-OH products would proliferate without the quality standards that some 7-OH makers and marketers appear to voluntarily adhere. An illicit 7-OH market also raises the potential, if not likelihood, of 7-OH products being replaced or adulterated with fentanyl related substances. While 7-OH’s potential benefits do not necessarily affect whether substances or products should be scheduled, these issues should be considered in how scheduling actions are implemented to minimize unintended individual and public health consequences. 5.4 Implications The widespread use of highly concentrated 7-OH products is a relatively new phenomenon in the U.S., but it appears to be growing rapidly. Since about 2022, data from surveillance systems and user reports from social media, surveys, and case studies provide valuable insights into the patterns of 7-OH use, with users reporting that they are using it for pain management, to self-treat opioid withdrawal, and for recreational purposes. Data from America's Poison Centers also indicate a growing public health problem, with a rising number of exposure cases involving 7-OH and serious health effects. The FDA has also issued warnings about the public health risks associated with 7-OH, citing the high concentrations of the substance in some products and the lack of regulation and quality control. It is important to note that 7-OH associated outcomes, both at the individual and population levels, have likely been underreported and instead attributed broadly to “kratom”. This underestimation arises because current surveillance methodology does not distinguish 7-OH products from traditional kratom preparations, instead aggregating them into a single “kratom” category. This problem is exacerbated by marketing and labeling of many 7-OH products as “kratom” or “kratom derived” with implied safety statements based on studies of kratom and its far more widely studied naturally occurring constituent, mitragynine. Page 33 of 128 Despite limitations, it is clear that 7-OH is becoming more of a concern and priority for regulatory, law enforcement, and surveillance authorities. Available evidence suggests that there are signals of meaningful real-world nonmedical use and abuse with potentially significant medical outcomes, such as dependence, withdrawal, and development of substance use disorder. However, it is still not clear the severity of the risk posed to the public health by 7-OH. While surveillance systems are capturing an increasing number of cases regarding kratom, this coincides with a rapidly growing kratom market with some estimates suggesting the total market size to be 1-1.5 billion USD. Presumably, a proportion of these cases are due to consumption of concentrated 7-OH products, as many of these cases have been included as “kratom” cases, though this figure is unclear based on current surveillance capabilities. For example, the 44th WHO Expert Committee on Drug Dependence (ECDD) reviewed the available evidence on kratom and its alkaloids in 2020 (UNODC, 2021). It concluded that there was insufficient evidence to recommend a critical review of these substances. However, the committee also noted the increasing availability of concentrated kratom products and the potential for these products to pose a public health risk. The UNODC has also issued an announcement about new kratom-related products, expressing concern about their potential health effects. However, this report was focused on kratom plant products and extracts and mitragynine studies and not the subcategory of high- concentration 7-OH products, which had not yet emerged as a significant or substantial category of product in the U.S. or globally. It is critical to characterize the relative risk of 7-OH to that of kratom products that are consistent with the natural constitution of the kratom plant, and to classical drugs of abuse. Despite a growing kratom market, there have been few signals of risk to the public health from natural kratom products, and a number of reports and surveys showing consumers using them for therapeutic purposes (Grundmann et al., 2022; Smith, & Lawson, 2017). FDA in its 2018 determination to rescind the recommendation for CSA control of mitragynine and 7-OH cited a “potentially substantial risk to public health if these chemicals were scheduled at this time” due to potential adverse consequences if kratom is no longer available for people using for symptoms such as intractable pain, psychological distress, risk for suicide, transition from opioids or other potential or harmful drugs (Giroir, 2018). Similarly, reported use of 7-OH includes consumers and patients using for therapeutic purposes, and who may suffer unintended adverse consequences from its sudden removal from the market. Given its distinct risk profile, especially in the context of highly concentrated 7-OH products, careful surveillance and research are necessary and warranted including but not limited to studying 7-OH using accepted FDA toxicological standards (e.g., through NIH funded research or through development as an FDA approved drug). 6 Factor 7: The Psychic or Physiological Dependence Liability As discussed in Factor 1 and elsewhere, this report agrees with FDA regarding the evidence that some 7-OH consumers can become psychologically and physically dependent and develop substance use and withdrawal disorders, respectively. However, the level of risk and an evidence-based characterization of 7-OH dependency, use disorder, or withdrawal has received little study and more research is warranted, Page 34 of 128 regardless of the scheduling action and approach. The existing data are likely to be considered insufficient to conclude at present that the 7-OH withdrawal syndrome is sufficiently similar to classical opioids to warrant inclusion in a diagnostic manual. 7 Factor 8: Whether the Substance is an Immediate Precursor of a Substance Already Controlled It is important to note that 7-OH does not meet the prototypical criteria of Factor 8 as an immediate precursor of a substance already controlled as it is neither an immediate precursor of a substance already controlled, nor is it an opioid based on its botanical origin or chemical structure. It is not an immediate chemical precursor used in the synthesis of any currently controlled substance. Furthermore, 7-OH is a metabolite of mitragynine, a naturally occurring alkaloid from the Mitragyna speciosa plant, which is botanically unrelated to the opium poppy (Papaver somniferum). Therefore, it is not an opiate derived by extraction or chemical synthesis from opium or its constituents, such as morphine or thebaine. However, the CSA includes a provision (21 U.S.C. § 802(18)) that guides determination of whether a substance can be determined to be sufficiently pharmacologically equivalent to morphine with respect to key effects related to “addiction liability” to be designated and regulated as an opioid. Specifically, no. 18 states: “The term ‘opiate’ or ‘opioid’ means any drug or other substance having an addiction-forming or addiction-sustaining liability similar to morphine or being capable of conversion into a drug having such addiction-forming or addiction- sustaining liability.” This pharmacological definition is critical to the regulatory consideration of 7-OH. It allows the DEA, upon recommendation from DHHS, to classify a substance as an opioid based on its effects, even if it does not meet the structural or precursor criteria of Factor 8. The determination of whether a substance has an “addiction-forming or addiction- sustaining liability similar to morphine” is based on the scientific and medical evidence evaluated under the other factors of the 8-FA, particularly Factors 1, 2, 3, and 7. An example of this in pharmaceutical development was tapentadol. During its evaluation and development as an analgesic, it was not designated as an opioid based on its chemical structure; however, based on its overall pharmacological profile and similarity to morphine and related opioids, tapentadol was placed in Schedule II of the CSA, along with morphine and oxycodone, following its approval for therapeutic use and is now widely classified as an “opioid”. 8 Scheduling Recommendation This 8-FA supports FDA’s preliminary July 29, 2025 recommendation that placement of 7-OH in the CSA is warranted. Moreover, because 7-OH has not been approved by FDA for therapeutic use and has not been determined by FDA and DHHS to be commonly accepted for medical use (i.e., CAMU), the only CSA scheduling option is Schedule I. Page 35 of 128 Specifically, the present analysis supports FDA’s “Assessment of the Scientific Data and Toxicological Concerns” which included the following conclusions: “Based on demonstrated pharmacology, repeated or prolonged use of 7-OH would lead to tolerance, physical dependence, and potentially to opioid addiction — typical of mu opioid agonist drugs of abuse.” The analysis of Factors 1, 2, 3 and 7 in the present report and the FDA analysis both support the conclusion that 7-OH meets the statutory criteria of the Controlled Substances Act’s specific provision (at 21 U.S.C. § 802(18)) that guides determination of whether a substance can be determined to be sufficiently pharmacologically equivalent to morphine with respect to key effects related to “addiction liability”. Thus, 7- OH can be designated and regulated as an opioid as discussed above in Factor 8. Moreover, with respect to the determination of whether 7-OH poses a known or imminent public health threat, which is among the criteria for both temporary (i.e., “emergency”) scheduling and permanent scheduling, FDA’s July 29th analysis concluded as follows: “The pharmacological profile, abuse liability, and emerging patterns of non- medical use establish 7-OH as a dangerous substance. Current regulatory gaps have enabled widespread availability of these products despite their opioid-like properties and necessitate immediate policy intervention to address this emerging threat to American public health.” Factors 4, 5, and 6 in the present report supports FDA’s conclusion that 7-OH poses a likely imminent public health threat, thus supporting the known or imminent public health threat criteria for temporary and permanent scheduling. 8.1 Policy Implementation Considerations to Minimize Unintended Consequences Evidence suggests that there is likely a proportion of individuals who may benefit from their use of 7-OH, with some considering it a life-saving path away from more deadly illicit opioids. While such reports may not, on their own, be sufficient justification to avoid scheduling 7-OH, they should be considered in how such a regulatory policy is implemented and enforced. As discussed in greater detail in the Research Priorities and Policy Considerations section below, some 7-OH consumers may need time, support, and assistance to identify effective alternatives, and to reduce the likelihood that a significant illicit market for 7-OH will emerge if 7-OH is scheduled. The FDA appeared careful in its July 29th documents and press conference to distinguish between concentrated 7-OH products and natural kratom products, which it acknowledges often contains detectable levels of 7-OH. For controlled substances the CSA does not set a level of for controlled substances that can be marketed without control. However, there are examples of substances and products that contain low levels of substances. For example, FDA has not banned, and DEA has not scheduled, poppy seeds used in cooking even though their consumption can produce detectable levels of morphine following consumption of poppy seed pastries, curries and other Page 36 of 128 foods. Other examples include a Parkinson’s Disease diagnostic scanning assay that includes small amounts of cocaine related substances that DEA determined did not require scheduling. Implementation may include a performance standard for kratom products such as the maximum allowable amount per serving size. As discussed in Factor 4, 5 and 6 and in the policy implications of this report, a subset of 7-OH users consider it to be their path away from illicit or pharmaceutical opioids that likely carry greater risks of overdose death than 7-OH. Individuals also report benefits such as relief of pain, sometimes describing 7-OH as more effective or preferred to FDA approved medicines or kratom. Although there are significant gaps in the current body of evidence that do not allow credible estimates of the incidence of such cases or the prevalence among 7-OH users, these reports underscore the importance of carefully planning and implementing any scheduling action. Enforcement priorities should aim to minimize the risks of 7-OH users relapsing to more deadly opioid use, and prevent the emergence of an illicit market in which trafficking organizations such as cartels manufacture and distribute unregulated 7-OH products. Such illicit products may lack the quality controls observed by at least some current manufacturers. Such illicit marketers may also add fentanyl related substances to 7-OH for boosted effects or even replace 7-OH with fentanyl related substances. To be clear, this discussion of potential unintended public health consequences does not mean that scheduling is not warranted; rather, it underscores the need for thoughtful implementation giving consideration to the potentially thousands of current 7-OH consumers. The timing, scope, and enforcement approach to scheduling and policy implementation should be carefully considered by the DEA/Department of Justice (DOJ) ideally in coordination with CDC, FDA, and NIH, with diverse stakeholder input (including 7-OH consumers). Such coordination would provide the umbrella of supporting surveillance, assistance, and research to detect and minimize unintended consequences, and provide time and assistance to current 7-OH users to find alternatives to 7-OH. 9 Research Priorities and Policy Considerations The recommendation by the FDA to the DEA of a scheduling action to control 7-OH under the CSA represents a significant federal response to what the agency has deemed an “emerging public health threat”. This action is a continuation of a complex history of regulatory considerations for kratom and its alkaloids and has continued to highlight gaps in the regulatory and legal framework for regulating novel botanical psychoactive substances. Some experts may feel that potentially lower real-world risks of addiction, abuse, and overdose exist for 7-OH and therefore warrant less restrictive scheduling than those drugs that are placed in Schedule II (i.e., fentanyl and oxycodone) and Schedule I (i.e., heroin). However, under current law, Schedule I is the only option for 7-OH. The CSA makes clear that if a drug has sufficient abuse potential to warrant scheduling and it is not approved by FDA or designated as CAMU, then placement in Schedule I is required. Further, while the evidence of overdose risk is primarily by the intravenous route and real world-use is primarily by the potentially lower risk oral route, the pharmacological Page 37 of 128 and toxicological profile of the ‘substance’ or ‘chemical entity’ is the basis for scheduling – regardless of route. If 7-OH is placed in Schedule I, and then in the future, a New Drug Application for a 7-OH containing product is developed and approved by FDA, that product will be removed from Schedule I and rescheduled or removed from CSA control as informed by an 8-FA for that product and other considerations. Specifically, as per the CSA, approved drugs are scheduled according to their abuse- related risks as guided by the 8-FA in which Schedule V is least restrictive (e.g., cough preparations with less than 200 milligrams of codeine or per 100 milliliters, and pregabalin) and Schedule II is most restrictive (e.g., morphine, oxycodone, amphetamine, cocaine and fentanyl). Thus, FDA’s report, “7-Hydroxymitragynine (7-OH): An Assessment of the Scientific Data and Toxicological Concerns Around an Emerging Opioid Threat”, summarizes the chemical, pharmacological and epidemiological evidence related to 7-OH safety and abuse potential. Although not structured as a formal 8-FA, it includes key data which formed the basis for its determination that: (a) 7-OH demonstrates sufficient pharmacological equivalence on key abuse and safety related variables to be considered an “opioid”, thus triggering CSA’s statutory implications that include placement in Schedule I if not approved as a drug, and placement in Schedule II if under development with an Investigational New Drug (IND) application that has been accepted; and, (b) 7-OH is “dangerous” and poses an imminent hazard to public health which satisfies a key criterion for temporary (aka “emergency”) drug scheduling. A critical implication of these two determinations is that to warrant scheduling, the substance does not need to carry the same or equivalent abuse potential or overdose risk as classical opioids (e.g., frequent reference standards morphine and oxycodone, or epidemiological comparators such as heroin and fentanyl). However, in practice, the greater the risk to public health, the greater the urgency and justification for rapid action. It is important to note that the definition of CAMU has been recently evolving, as evidenced by the 2024 DEA recommendation to place marijuana into Schedule III of the CSA (DEA, 2024), which states: “In its most recent evaluation, HHS informed DEA of its view that DEA's previous approach to determining whether a drug has a CAMU does not adequately account for certain indicia of medical use that, where present, are relevant to determining whether a substance has a CAMU for purposes of scheduling under the CSA. Specifically, HHS observed that DEA's tests left no room for an evaluation of (1) whether there is widespread medical use of a drug under the supervision of licensed health care practitioners under State-authorized programs and, (2) if so, whether there is credible scientific evidence supporting such medical use.” DHHS therefore developed an alternative test wherein: Page 38 of 128 “Under Part 1 of the HHS CAMU test, the Office of the Assistant Secretary for Health (“OASH”) considered whether there is widespread current experience with medical use of marijuana in the United States by licensed [healthcare providers] HCPs operating in accordance with implemented State-authorized programs, where such medical use is recognized by entities that regulate the practice of medicine under these State jurisdictions. Part 2 of the CAMU test evaluated whether there exists some credible scientific support for at least one of the medical conditions for which the Part 1 test is satisfied. The evaluation in Part 2, undertaken by FDA, was not meant to be, nor is it, a determination of safety and efficacy under the Federal Food, Drug, and Cosmetic Act's drug approval standard for new human or animal drugs. Rather, HHS's two-part test is designed to evaluate whether a substance, in this case marijuana, has a CAMU for purposes of drug scheduling recommendations and placement in a drug schedule consistent with criteria set forth in 21 U.S.C. 812(b).” While there are reports of consumers using 7-OH for therapeutic purposes, the available body of evidence falls far short of the level that supported DHHS/FDA designation of “marijuana” as CAMU in its 2023 analysis, led by the Office of the Assistant Secretary of Health (OASH). The analysis included extensive data which confirmed “that more than 30,000 HCPs [health care providers] across 43 U.S. jurisdictions are authorized to recommend the medical use of marijuana for more than six million registered patients for at least 15 medical conditions. OASH’s Part 1 analysis, therefore, supports the finding that marijuana has at least one CAMU in the United States.” Note this evaluation does not mean marijuana has been approved as a drug for any given condition. Rather, the widespread and well-documented medical use was deemed sufficient to satisfy the CAMU requirement and provide the basis for removal of marijuana from Schedule I – a recommendation that is presently under consideration by the DEA. Currently, no comparable body of evidence exists to support a similar CAMU designation for 7-OH Likewise, neither kratom nor any of its alkaloids (including mitragynine, the predominant active constituent in most kratom products and extracts) have been designated as CAMU. Further, kratom and its alkaloids have not been designated as ‘opioids’ based on botanical origin, chemical structure, or sufficient pharmacological equivalence to morphine. Moreover, several prior 8-FAs have determined that they do not warrant scheduling under the Controlled Substances Act. This includes the 2018 analysis by Assistant Secretary Brett Giroir (Giroir, 2018), which rescinded an earlier recommendation to schedule kratom's main alkaloids, mitragynine and 7-OH. That rescission was based on the determination that the scientific evidence at the time was underdeveloped and insufficient, and that scheduling carried a “significant risk of immediate adverse public health consequences,” such as driving users to more lethal opioids. Similarly, the in 2020, the World Health Organization's Expert Committee on Drug Dependence (ECDD), found insufficient evidence to recommend a critical review of kratom, mitragynine, and 7-OH for international scheduling, though it recommended continued surveillance (UNODC, 2021). Three other 8-FA (one submitted as a comment Page 39 of 128 to DEA in 2016 [Henningfield and Fant, 2016], and two as peer reviewed publications (Henningfield, Fant, and Wang, 2017; Henningfield, Wang, and Huestis, 2021) also concluded that kratom did not warrant CSA scheduling. Although these prior evaluations included consideration of 7-OH, they did not find sufficient basis for scheduling at the time. However, the science has advanced significantly in recent years as discussed in Factor 3. Specifically, the introduction to Kratom: History, Science, and Therapeutic Potential, a recently published book featuring contributions from many of the world’s leading kratom researchers, notes the rate of annual kratom science publications increased from about 20 per year in 2016 to more than 130 per year by 2024, with the increased fueled heavily by research funding by the National Institutes of Health (NIH), NIDA (Henningfield, Beyer, & Raffa, 2025). The rapid growth in 7-OH marketing and consumption since 2022, coupled with an expanding body of research addressing its abuse potential and safety (Reissig et al. 2025), in addition to the increased body of evidence regarding kratom in general, has altered the public health context. Accordingly, this report concurs with the July 2025 FDA’s evaluation that potential and increasing public health risks – exacerbated by extensive 7-OH product marketing and consumer consumption, rising consumer exposure, and new scientific evidence – support the recommendations for scheduling. As discussed earlier, the foregoing observations of this report and those of Reissig et al. above are consistent with recent conclusions and evaluations by other experts which suggest that some fraction of the adverse events and possibly deaths that have been reported and or interpreted as involving or even caused by kratom, were actually more likely attributable to the consumption of 7-OH products in addition to or in place of kratom (Grundmann et al., 2024; Hill, Boyer, et al., 2025; Papsun et al., 2023; Smith et al., 2025; Vadiei, Evoy, & Grundmann, 2025). Taken together, the foregoing observations support the conclusion that it is urgent to add 7-OH to relevant substance surveillance systems including NSDUH, RADARS, FAERS, and poison control. Similarly, assessment of 7-OH in blood plasma in forensic toxicology examinations as well as kratom research in general is a critical need. As discussed in Factor 5, it is beyond the scope of this report to specify how surveillance systems should be designed to distinguish between kratom products and those containing 7-OH, including the precise wording of survey questions or the analytical methods to detect 7-OH, which should be developed with input from appropriate experts and stakeholders. 9.1 Comparison of 7-OH to Kratom and other Substances Currently, many kratom and related products, including concentrated 7-OH products are marketed as dietary ingredients and/or supplements, though to date no NDIN has been accepted by FDA and the lack of documented history of use prior to 1994 has precluded its acceptance as an ingredient exempt from the NDIN requirements as described in the Dietary Supplement Health and Education Act (DSHEA) of 1994. A crucial aspect to determine 7-OH’s risk to the public health is the distinction between traditional kratom and concentrated 7-OH products. The FDA has explicitly stated that its primary concern Page 40 of 128 is not with natural kratom leaf, where 7-OH is present in only trace amounts, but with the “concentrated 7-OH opioid products” that are ‘far more dangerous”. While traditional kratom is not without risks and has been associated with dependence and adverse events, its risk profile appears to be substantially lower than that of concentrated 7-OH. The limiting nature of consuming bulky plant powder and the complex interplay of dozens of alkaloids in traditional kratom may moderate its effects and abuse potential compared to isolated 7-OH. However, neither these statements from FDA nor kratom’s apparent lack of signal of risk to public health should be misinterpreted that the Agency accepts kratom as safe. It has not accepted any submitted NDINs in which the standard for acceptance is that the products specified in the NDIN’s were found to be “acceptably safe”, though this has not been a standard that FDA has formally defined. In December 2023, FDA stated in a federal court hearing in the Southern District of California that the Agency had not yet determined if kratom was hazardous (United States v. Nine2Five, LLC, No. 3:23-CR- 00179-TWR [S.D. Cal.], ECF No. 110-8). FDA also reminds the public on its kratom website page that kratom has not been approved for therapeutic use. While this is not directly relevant to the legality or safety of kratom as approval for therapeutic use is not a standard for accepting a substance as a dietary substance, it means that products cannot legally be marketed with disease treatment and prevention claims. When compared to illicit opioids, FDA describes the risk of 7-OH as a potential “new wave of the opioid epidemic”, and implies the potential risk of fueling an overdose epidemic rivaling that by three earlier waves of prescription drugs, heroin, and fentanyl (and related substances) - a message reinforced by recent pharmacological and epidemiological data presented by FDA (Reissig et al., 2025) and portrayed in a graphic in its educational materials (FDA, 2025b). 9.2 Potential Unintended Consequences of Schedule I Placement and Policy Implications 9.2.1 Potential Unintended Consequences of Scheduling While scheduling 7-OH under the CSA is intended to mitigate public health risks, such an action has the potential to create unintended negative outcomes. A comprehensive policy analysis must consider potential unintended consequences, which could, in some cases, undermine the primary goal of protecting public health. 9.2.1.1 Relapse by Patients and Consumers to Harmful Opioids A key consideration in the 2018 DHHS decision not to schedule kratom or its alkaloids was the concern that a ban would cause individuals using kratom to manage opioid withdrawal symptoms or chronic pain to switch to more dangerous and harmful substances such as heroin and fentanyl (Giroir, 2018). These risks and others described by Giroir (see also Henningfield, Fant and Wang (2018); Henningfield, Grundmann, et al. (2019); Henningfield and Fant (2016)) appear plausible if 7-OH is scheduled. Page 41 of 128 As discussed in Factor 6 of this report, a similar conclusion as pertains to 7-OH is based on admittedly limited anecdotal evidence suggesting that some 7-OH users report that 7-OH to be more effective, acceptable, or assessable than FDA approved medicines, kratom, or other approaches, as was similarly concluded for kratom in 2016 (Henningfield and Fant, 2016), and in subsequent analyses (Giroir, 2018; UNODC, 2021). Nonetheless, it is foreseeable that removal of 7-OH from the licit marketplace carries the risks of unintended consequences of 7-OH consumers relapsing to potentially deadlier opioid use, and resulting in an illicit market in which 7-OH products would proliferate without the quality standards that some 7-OH makers and marketers appear to voluntarily adhere. An illicit 7-OH market also raises the potential if not likelihood of 7-OH products being replaced or adulterated with fentanyl related substances. This risk is not theoretical and decades of experience with opioids have elucidated what is sometimes referred to as the “whack A mole” effect, whereby reduction in access to one opioid has little effect on overall opioid use as people simply migrate to other opioids. Thus, for example, when the abuse deterrent formulation of OxyContin was marketed in August 2010 and the original OxyContin removed from the market, OxyContin abuse actually decreased. However, surveillance studies over the next two years revealed there was no reduction in opioid use but rather use of other opioids (including fentanyl and hydromorphone selection) rose markedly from 20% to 32% and heroin use nearly doubled (Cicero, Ellis, & Surratt, 2012). Even more sobering is that although high dose and Schedule II opioid prescribing rates have declined in the U.S. since about 2012, annual opioid overdose deaths have continued to increase primarily due to heroin and fentanyl related substances (Henningfield, Ashworth, et al., 2019; Strickler et al., 2020). 9.2.1.2 Restrictions and Impediments to Scientific Research Placing 7-OH in Schedule I would impose significant regulatory barriers on scientific research. Investigators wishing to study the substance – whether for its risks or its potential therapeutic benefits – would face stringent registration, security, and record- keeping requirements from the DEA, as well as funding limitations in procuring, storing, or administrating these substances in research settings (Andreae et al., 2016). This could stifle much-needed research into 7-OH's pharmacology, safety profile, and potential as a lead compound for developing safer analgesics. The G-protein biased agonism of 7-OH is of significant scientific interest for the development of novel pain medications with fewer side effects, and a Schedule I designation could severely hamper progress in this area. 9.2.1.3 Criminalization and Enforcement Placement in Schedule I could have profound consequences including potentially severe restrictions and criminal penalties for possession and distribution. As the benefits and risks of 7-OH and the extent to which consumers are using 7-OH for therapeutic purposes have yet to be determined, it’s important for policy decisions to consider the actions and effects that may have potential unintended consequences and how to minimize the risks. Page 42 of 128 While there are no reliable estimates of how many people use 7-OH for therapeutic purposes, the potentially thousands of people using 7-OH to refrain from harmful opioid use may benefit from additional federal resources, funding treatment and harm reduction for substance use issues, as well as the DOJ deprioritizing individual possession while prioritizing inappropriate marketing and sales. The specific options and approaches for policy to minimize unintended consequences are beyond the scope of this report; however, this report recommends consideration should be given to risk mitigation before 7-OH is scheduled. A request for comment and possibly a public hearing to give consumers and various important stakeholders consideration is recommended, because preliminary anecdotal reports suggest that for some people 7- OH is their lifeline away from potentially more deadly opioid such as fentanyl. 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Published Findings Related to Abuse, Physical Dependence, Withdrawal, and Safety Signals of 7-OH Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Factor 1: Actual or Relative Potential for Abuse Gonzalez et al. (2025) Mitragynine and 7- Hydroxymitragyni ne: Bidirectional Effects on Breathing in Rats. MG: 5.6, 10, 17.8 mg/kg, IV 7-HMG: 1, 3.2, 10 mg/kg, IV Positive control opioid: morphine (10, 32 mg/kg IV). Antagonist: naloxone (1 mg/kg IV). NA Did not assess withdrawal Morphine caused dose- dependent respiratory depression while mitragynine unexpectedly increased respiratory frequency at 10 mg/kg, with no significant depression of tidal/minute volume. High dose (17.8 mg/kg) caused seizures in some rats without respiratory depression. MG’s stimulant effect was not blocked by naloxone, suggesting a non- opioid mechanism. 7-OH-MG caused dose- dependent respiratory depression: reduced frequency and minute volume at 3.2 and 10 mg/kg, tidal volume trends toward depression. Naloxone fully reversed 7-HMG-induced respiratory depression (tidal and minute volume restored). NA Sudmoon et al. (2025) Discovery of rhynchophylline and mitraphylline in two Thai Toxicity testing of two Thai Mitragyna species and the investigation of their biological activity via opioid MG, 7-OH-MG, mitraphylline, and rhynchophylline NA NA Mild motor impairment seen at ≥50 mg/kg IP, no lethal effects MG exhibited moderate affinity for the MOR and KOR, whereas 7-OH- MG had 14x greater binding affinity than MG. Rhynchophylline, MG, and 7-OH- MG were found in other Mitragyna species. Page 54 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Mitragyna species and the investigation of their biological activity via opioid gene expression analysis. gene expression analysis Henningfield, Rodricks, et al. (2022) Rat respiratory effects & plasma MG & 7-OH-MG Oxy & MG General behavior (e.g., sedation) NA Oxy: respiratory depression & deaths; MG: no respiratory effect Plasma MG & 7-OH-MG confirmed high-dose exposure. Chakraborty, Uprety, et al. (2021) Oxidative metabolism as a modulator of kratom’s biological actions MG, 7-OH-MG, MGP 7-OH-MG & MG showed significant CPP, though MGP did not NA 7-OH-MG inhibited GI transit. 7-OH-MG produced from MG via CYP3A mediated oxidation. Acts as a MOR agonist and produced dose-dependent antinociception in tail flick and hot plate. Higher potency by the oral route vs morphine which was higher via SC admin. Obeng et al. (2021) Pharmacological comparison of Mitragynine and 7-OH-MG DAMGO, morphine, fentanyl, buprenorphine, nalbuphine, naltrexone, U69,593; SNC-80 MG, 7-OH-MG 7-OH-MG produced a maximum of 100% drug lever responding in morphine trained rats In MG-trained rats, 7-OH-MG produced a maximum of NA 100 mg/kg MG lethal (IP), even with 10 mg/kg naltrexone. 7-OH-MG produced significant naltrexone- and naloxone-reversible antinociception in rats in hot plate test. Page 55 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments 98% drug lever responding Gutridge et al. (2020) G protein-biased kratom-alkaloids and synthetic carfentanilamide opioids as potential treatments for alcohol use disorder Kratom extract, mitragynine, paynantheine, speciogynine, 7-OH- MG (3 mg/kg, IP) MP102, MP103, MP105, TRV130 morphine, DAMGO, Leu-enkephalin, U50,488 CPP findings show reward potential for kratom extract and 7-OH-MG NA NA MG, paynantheine, and speciogynine reduced ethanol intake at 10-30 mg/kg in mice. 7-OH-MG reduced intake at 1-3 mg/kg (male) and 3 mg/kg (female). Speciogynine (30 mg/kg) decreased activity. 7-OH-MG (3 mg/kg) increased locomotor activity. Kratom extract #1 (30 mg/kg) and 7- OH-MG (3–10 mg/kg) induced CPP. Morphine induced CPP as expected. Obeng et al. (2020) Adrenergic and opioid binding affinities, metabolic stability, plasma protein binding properties, and functional effects of selected indole-based kratom alkaloids MG, 7-OH-MG, speciociliatine, corynantheidine, 9- hydroxycorynantheid ine NA NA NA 7-OH-MG had the highest affinity among tested alkaloids at the MOR, and showed high affinity at the KOR and moderate affinity at the DOR. In rat hot plate tests, 7-OH-MG produced greater potency than morphine and speciociliatine but lower than fentanyl. Analgesic effect blocked by naltrexone. Did not produce hypothermia. Todd et al. (2020) Receptor binding of 7-OH-MG, 7-OH-MG, mitragynine, speciofoline Binding affinity to opioid receptors NA Not population-specific MG and 7-OH function as partial agonists of the human MOR, while speciociliatine does not exhibit measurable binding affinity at the Page 56 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments mitragynine, and speciofoline MOR, DOR, or KORs. MG and 7-OH demonstrate functional selectivity for G-protein signaling, with no measurable recruitment of β- arrestin. Hemby et al. (2019) Abuse liability and therapeutic potential of the Mitragyna speciosa (kratom) alkaloids mitragynine and 7- hydroxymitragyni ne. MG: 25-150 µg/infusion, 7-OH-MG: 2.5-20 µg/infusion Morphine: 50-100 µg/infusion Experiment 1: MG did not substitute for morphine at any dose. 7-OH-MG substituted for morphine in a dose- dependent manner (2.5– 20 µg/infusion), with an inverted U- shaped curve and maximal response at 5– 10 µg/infusion Experiment 2: Morphine and 7-OH-MG both engendered and maintained self admin. MG did not NA No lethality reported NA Page 57 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments 7-HMG maintained intake at 2.5- 10 µg/infusion, comparable to morphine Experiment 3: Morphine intake reduced by NLXZ (μ1 antagonist) but not NTI. 7-HMG intake reduced by both NLXZ and NTI, suggesting reinforcement mediated by MOR and DOR. Kruegel et al. (2019) Hydroxymitragyni ne is an active metabolite of mitragynine and a key mediator of its analgesic effects. MG, 7-OH-MG, MGP NA NA NA MG is converted in vitro in both mouse and human liver preparations to 7-OH-MG, mediated by CYP P450 3A 7-OH is formed from MG in mice and that brain concentrations of this metabolite are sufficient to explain most or all of the opioid-receptor- mediated analgesic activity of MG. At the same time, MG is found in the brains of mice at very high concentrations relative to its opioid Page 58 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments receptor binding affinity, suggesting that it does not directly activate opioid receptors. Kruegel et al. (2016) Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators MG, paynantheine, speciogynine, speciociliatine, 7- OH, morphine, DAMGO, fentanyl, HEK293 Characterizatio n of 7-OH's activity at MOR, KOR, DOR. 7-OH-MG bound MOR with high affinity (Ki ~ 30 nM). Showed G- protein biased signaling NA Both 7-OH and MG were found to elicit no measurable β-arrestin recruitment 7-OH-MG produced potent antinociception, 10x more potent than morphine, blocked by naloxone. At equianalgesic doses, 7-OH-MG caused less respiratory depression and constipation than morphine. Harun et al. (2015) Discriminative stimulus properties of mitragynine (kratom) in rats. MG: 3-56 mg/kg IP), 7-HMG: 0.3–3 mg/kg IP, Morphine, codeine, cocaine, diazepam, U50,488H MG did not substitute for morphine. 7-OH-MG fully substituted for morphine. Effects were dose dependent and naloxone reversible NA No lethal toxicity. MG at high doses produced sedation and reduced response. 7-OH-MG elicited responses at much lower doses (0.3-3 mg/kg). NA Matsumoto et al. (2004) Antinociceptive effect of 7-OH- MG in mice 7-OH-MG, MG, morphine NA NA No safety-related signals or adverse effects reported 7-OH-MG showed dose-dependent antinociceptive properties when subcutaneously and orally administered to mice. Also suggests Page 59 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments 7-OH-MG may be more orally bioavailable than morphine. Factor 2 Scientific Evidence of its Pharmacological Effects J. P. Manus et al. (2025) Effects of kratom alkaloids on mesolimbic dopamine release. MG, 7-OH-MG, (cocaine, amphetamine, opioids mentioned but not directly compared) NA NA NA Fixed potential amperometry was used to quantify stimulation-evoked phasic dopamine release in the nucleus accumbens (NAc) of anesthetized male and female mice before and after MG (1, 15, or 30 mg/kg, IP), 7-OH-MG (0.5, 1, or 2 mg/kg, IP), or vehicle. MG reduced dopamine release over the recording period (90 min) in a dose-dependent manner, and the low dose of MG significantly increased dopamine autoreceptor functioning in males. Both sexes responded similarly to 7- OH-MG with the low dose of 7-OH- MG increasing dopamine release while the high dose decreased dopamine release. 7-OH-MG did not alter dopamine autoreceptor functioning for either sex. Neither MG nor 7-OH-MG altered the clearance rate of stimulation-evoked dopamine. Findings suggest that these kratom alkaloids do alter dopamine functioning, although potentially not in a way consistent with classic drugs of abuse. Page 60 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Obeng et al. (2022) Interactive Effects of m- Opioid and Adrenergic a2 Receptor Agonists in Rats Pharmacological investigation of the primary kratom alkaloid mitragynine and its metabolite 7- hydroxymitragyni ne MG, 7-OH-MG, morphine, methadone, clonidine, lofexidine, U69,593, naltrexone, yohimbine MG showed low affinity at α2A and α2C receptors MG bound MOR with Ki ~1700 nM. 7-OH-MG showed stronger MOR affinity (Ki ~78 nM) but no α2 binding at ≤10 μM. NA No toxicity or lethality reported. MG has weak affinity for MOR but meaningful interactions with α2- adrenergic systems. Combined activity may account for kratom’s mixed reported stimulant/analgesic profile. In hot plate tests, MG did not produce significant antinociception across routes (IP, SC, oral). In contrast, 7-OH-MG produced robust, naloxone-sensitive antinociception. MG and 7-OH-MG enhanced potency of α2 agonists (clonidine/lofexidine) Maxwell et al. (2021) Oral pharmacokinetics in beagle dogs of the mitragynine metabolite, 7- hydroxymitragyni ne. MG, 7-OH-MG NA NA NA Following a single oral dose (1 mg/kg) of 7-HMG, plasma samples were obtained from healthy female beagle dogs. Absorption of 7-HMG was rapid, with a peak plasma concentration (Cmax, 56.4 ± 1.6 ng/mL) observed within 15 min post-dose. In contrast, 7- HMG elimination was slow, exhibiting a mono-exponential distribution and mean t1/2 of 3.6 ± 0.5 h. Oral dosing of 1 mg/kg 7- HMG was well-tolerated with no observed AEs or significant changes to clinical laboratory tests. The exposure of 7-HMG after MG dosing due to metabolism corresponds to a 0.24 mg/kg dose of 7-HMG indicating a 23.1% Page 61 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments conversion of MG to 7-HMG in beagle dogs. Ellis et al. (2020) Receptor binding and signaling of kratom MG, 7-OH-MG, other alkaloids Binding affinity to opioid receptors NA Not population-specific Identified MOR partial agonism for 7-OH-MG and MG, biased signaling. Takayama et al. (2002) Synthesis and Opioid Agonistic Activities of Mitragynine- Related Indole Alkaloids MG, 7-OH-MG, pseudoindoxyl Morphine NA NA NA In vitro tissue assays and in vivo mouse hot plate and tail-flick tests showed potent naloxone reversible antinociception Factor 3 Current State of Scientific Knowledge Akbar et al. (2025) Screening, docking, and molecular dynamics analysis of Mitragyna speciosa (Korth.) compounds for targeting HER2 in breast cancer. MG, 7-OH-MG, paynantheine, speciociliatine, speciogynine NA NA NA MG was found to be BBB permeant, whereas 7-OH-MG was not BBB permeant, which could reduce the likelihood of CNS-related side effects. Neither were found to be P-gp substrates, which minimizes the risk of efflux-related bioavailability issues. However, both were inhibitors of CYP2D6 and CYP3A4 enzymes. 7-OH-MG demonstrated MOR binding and partial agonist activity. 7-OH-MG showed potent G-protein biased MOR agonism. Page 62 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments 7-OH-MG and MG both demonstrated high GI absorption, suggesting high oral bioavailability. Docked to HER2 binding pocket with lower binding energies, and 7-OH- MG demonstrated stable hydrogen- bond interactions with residues critical for HER2 inhibition. Chiang et al. (2025) In Vitro and In Vivo Pharmacokinetic Characterization of 7- Hydroxymitragyni ne, an Active Metabolite of Mitragynine, in Sprague-Dawley Rats. MG MGP, 7-OH-MG NA NA NA 7-OH-MG exhibited high permeability in Caco-2 cells 7-OH-MG exhibited lower plasma protein binding in rats compared to MTG. Lower plasma protein binding of 7-OH-MG may lead to a larger volume of distribution and a shorter t1/2 than MTG. 7-HMG showed a rapid elimination with short metabolic half-lives in rat liver microsomes (0.4 ± 0.0 h) and hepatocytes (0.3 ±0.0 h). After oral dosing, the Cmax was 28.5 ± 5.0 ng/ml, and Tmax was 0.3 ± 0.1 h, which indicated rapid absorption of 7-HMG. The t1/2 of 7-HMG was 0.5 ± 0.0 and 1.7 ± 0.5 h after IV and oral dosing, respectively, which indicated 7-HMG eliminates rapidly from the systemic circulation. In contrast to other studies, this study found poor oral bioavailability Page 63 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments of 7-OH-MG, though this may be due to poor water solubility. The concentration of 7-HMG fell below the LLOQ after 8 h following IV administration and 4 h following oral administration. Uchaipichat (2025) Inhibitory effects of Kratom constituents, mitragynine and 7- hydroxymitragyni ne, on 4- methylumbellifer one glucuronidation by human UDP- glucuronosyltran sferases. MG, 7-OH-MG NA NA NA 7-OH exhibited the highest inhibitory potency on UGT1A9, with IC50 value of 51 µM, while moderate potency was observed for UGT1A1 and UGT1A3, with IC50 value of 196 and 141 µM, respectively. The inhibitory potency of 7-OH on UGT2B15 was low (IC50 > 200 µM), while negligible effects were observed for UGT1A6 and UGT2B7. 7-OH competitively inhibited UGT1A3 (Ki = 33 µM) and noncompetitively inhibited UGT1A9 (Ki = 29 µM). Values are relatively high compared to the maximum plasma concentrations reported in humans, suggesting an unlikely potential for herb-drug interactions via UGT inhibition. Berthold et al. (2024) Pharmacokinetic Interaction of Kratom and Cannabidiol in Male Rats MG, 7-OH-MG, speciociliaine, paynantheine, speciogynine, corynantheidine measured NA NA NA The metabolite to parent (i.e., mitragynine) exposure ratio percentage of 7-OH-MG remained similar (3.5 and 3.1 with and without cannabidiol, respectively). As there was an increase in MG exposure during this study, it was expected that this would be due to a decrease Page 64 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments OPMSS Gold kratom extract (11.8 mg/mL MG, 2.8 mg/mL speciociliatine, 2.2 mg/mL paynantheine, 1.5 mg/mL speciogynine). CBD (33.3 mg/mL cannabidiol) in metabolism, but this was not the case for 7-OH-MG despite it being primarily metabolized by CYP3A and cannabidiol being a competitive inhibitor of CYP3A Chiang et al. (2024) Multiple-Dose Pharmacokinetic s and Safety of Mitragynine, the Major Alkaloid of Kratom, in Rats. MG, 7-OH-MG (Morphine, oxycodone, methadone mentioned but not directly compared) NA NA NA Female rats showed significantly higher exposure to 7-OH-MG compared to male rats after multiple doses of MTG; similar results in mice (may not be applicable to humans, as women have higher expression of CYP3A activity than men); whereas male rats have higher expression than female rats. Huestis et al. (2024) Human Mitragynine and 7- Hydroxymitragyni ne Pharmacokinetic s after Single and Multiple Daily Doses of Oral Encapsulated Dried Kratom Leaf Powder. Kratom leaf powder Measured MG and 7-OH-MG NA COWS and SOWS No opioid-like withdrawal observed after cessation of either single or 15 day dosing. Mild AEs including GI upset (vomiting, nausea), dizziness, fatigue. No serious AEs reported. Hematology, liver/kidney panels normal. Controlled clinical PK study of kratom leaf capsules — first large double-blind, placebo-controlled trial with single and repeated dosing Mean metabolite ratio of 7-OH-MG ranged from 21-31% after a single oral dose of kratom capsules (MTG content 6.7-53.2mg) and 15-18% after multiple doses of kratom. Page 65 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Mongar et al. (2024) Effects of Itraconazole on Pharmacokinetic s of Mitragynine and 7- Hydroxymitragyni ne in Healthy Volunteers. Kratom tea, MG, 7- OH-MG NA NA Only single dose study, no tapering or withdrawal monitoring Total of 15 AEs were recorded during period 1: drowsiness (56.2%), vomiting (31.2%), dizziness (31.2%), headache (18.7%), fatigue (18.7%), and nausea (12.5%), while other typical AEs such as diarrhea, fever, skin itchy, irritation, constipation, anorexia, and heartburn were not observed. In period 2, the only AE observed was vomiting (6.3%). All events were resolved on the same day without any treatment and did not lead to any drop outs After oral administration of kratom tea (MTG content 23.6 mg), the mean metabolite ratio of 7-OH-MG was 11.5-16.2%. The median Cmax for MTG of 159.12 ± 8.68 ng/mL was attained in 0.84 h. While median Cmax for 7-OH of 12.81 ± 3.39 ng/mL was observed at 1.77 h. Tanna et al. (2022) Clinical Pharmacokinetic Assessment of Kratom (Mitragyna speciosa), a Botanical Product with Opioid-like Effects, in Healthy Adult Participants Kratom tea from purified Mitragyna speciosa (2 g) NA NA Kratom tea was well-tolerated in 5 of 7 enrolled participants. 2 participants experienced nausea and vomiting; 1 withdrew due to these AEs, and 1 was withdrawn due to abnormal appearing urine deemed likely unrelated to kratom consumption. 2 participants experienced lightheadedness and headache, deemed unrelated to kratom and related to placement of IV catheter. PK results of 3S and 3R alkaloids included the following: Plasma concentrations for 3S/3R alkaloids were quantifiable 15 min after consumption, suggesting rapid absorption. Multiple peaks during absorption reflected delayed GI emptying common with opioids. Minimal 3S/3R alkaloids were excreted unchanged in urine. 3S alkaloids (MG, speciogynine, and paynantheine) followed biphasic concentration-time profile; displayed higher peripheral volumes of Page 66 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments No patients experienced severe AEs. distribution and clearance than 3R alkaloids; exhibited longer terminal t1/2, higher CL/F and Vz/F, lower dose-normalized AUCinf and Cmax, shorter Tmax than 3R alkaloids. 3R alkaloids (mitraciliatine, speciociliatine, isopaynantheine) followed monophasic concentration- time profile. Kamble et al. (2021) Pharmacokinetic s of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats Traditional Kratom (lyophilized kratom tea) Commercial Kratom (OPMS liquid shot) NA NA NA Among the 11 alkaloids, only MG, 7- OH-MG, speciociliatine, and corynantheidine showed systemic exposure 8 h postdose, and the dose-normalized systemic exposure of these four alkaloids was higher (1.6−2.4-fold) following the administration of the commercial OPMS liquid. Paynantheine and speciogynine levels were quantifiable up to 1 h postdose, whereas none of the other alkaloids were detected. Hiranita et al. (2020) Potential Contribution of 7- Hydroxymitragyni ne, a Metabolite of the Primary Kratom (Mitragyna Speciosa) Alkaloid Mitragynine, to the μ-Opioid Activity of MG and 7-OH binding activity and efficacy at the MOR were compared Plasma levels following PO MG administration were measured Antinociception in In rats discriminating morphine (3.2 mg/kg, IP) from vehicle, the discriminative stimulus effects of MG were assessed 90 min after PO administration. NA 32 mg/kg MG was lethal. Binding activity of 7-OH at MOR (Ki = 78 nm) was 22-fold lower than morphine and 9-0 fold higher than MG. Following PO administration of MG (HCl salt, 55 mg/kg), Cmax of 7-OH (85 ng/mL) was 14-fold less than MG. Tmax of 7-OH and MG were 30 and 84 min, respectively. 7-OH is a more potent and efficacious MOR agonist than MG, Page 67 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Mitragynine in Rats hotplate assay was assessed MG (up to 178 mg/kg) produced 76% morphine-lever responding (ED50=51 mg/kg). suggesting that conversion to this metabolite may contribute to the in vivo MOR of MG. Kamble et al. (2020) Metabolism of a Kratom Alkaloid Metabolite in Human Plasma Increases Its Opioid Potency and Efficacy 7-HMG in pooled mouse, dog, monkey, and human plasma was evaluated NA NA NA Stability varied across species with high stability in mouse, rat, and monkey plasma (>80% 7-HMG remained after 120 min), intermediate stability in dog plasma (>61% remaining after 120 min), and low stability in human plasma (~40% 7-HMG remaining after 120 min). Incubation of human plasma produced an unknown converted metabolite with NMR data matching MGP. Study findings suggest potential for human plasma to form MGP. Factor 4 History and Current Patterns of Abuse Factor 5 The Scope, Significance and Duration of Abuse Factor 6 What, if any, Risk is there to the Public Health Broul et al. (2025) Case Report: Cannabis and kratom-induced self-amputation of ears and penis. NA NA NA NA 31 year old suffered severe substance-induced psychosis involving kratom and cannabis that resulted in self-amputation. Page 68 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Grundmann et al. (2025) Prevalence and Use Patterns of Kratom (Mitragyna speciosa Korth.) in a US Nationally Representative Sample. NA NA NA Adverse events more frequently reported with gummies/capsules/tablets/pill s at higher doses No 7-OH-MG specific data Survey of 11,545 respondents, 1,049 current kratom users (9.1% prevalence) Motivations for use (among users): Pain relief: 57.5% (n=603). Relaxation/stress relief: 53.6% (n=562). Energy boost: 49.6% (n=520). Higher reported frequency of kratom shots/extract powder consumed was correlated with use for pain relief Hill, Boyer, et al. (2025) De facto opioids: Characterization of novel 7- hydroxymitragyni ne and mitragynine pseudoindoxyl product marketing. 7-OH-MG, MGP NA NA Did not assess withdrawal directly, but authors noted widespread online reports of 7-OH-MG dependence and withdrawal Identified 304 marketed 7-OH and/or MGP products. 82.2% = 7-OH alone. 14.5% = 7-OH + MGP combos. 3.3% = MGP alone. Formulations: chewable/sublingual tablets (60.2%), liquid shots (20.7%), gummies (4.3%), drink mixes (4.0%), vapes (3.0%), syrups (2.3%), capsules (2.0%), strips (2.0%), food (1.3%), powder (0.3%). Claims: 73.4% made “general wellbeing” claims (focus ↑ 58%, relaxation 47%, energy boost 39%). Page 69 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments 37.8% made “functional” claims (pain relief 26%, anxiety/stress reduction 21%). 12.5% made explicit “drug” claims (opioid receptor activity, analgesia, sedation). Dosing/costs: Recommended dose range = 1-700 mg; mean = 20 mg/dose (7-OH higher than MP). MP mean recommended dose = 10.1 mg. Mean cost per recommended dose = $3.97 (7-OH); ~$5 for MP. Marketing: 93.1% falsely marketed as “kratom” despite being semi- synthetic opioids. Many brands mimic prescription medications (names like “Curevana,” “Pain Crusher Rx,” packaging like blister packs or syrups). Osawa and Johnson (2025) Postmortem distribution of mitragynine and 7- hydroxymitragyni ne in 51 cases Fluid and tissue specimens from 51 postmortem cases to investigate the distribution of MG and its active metabolite 7-OH. NA NA NA Central and peripheral blood concentrations were compared, with an average heart blood to femoral blood ratio being 1.37 for MG and 1.08 for 7-OH. This ratio >1.0 suggests that MG has some propensity toward postmortem redistribution; however, the difference in concentrations of MG and 7-OH was not statistically significant. Page 70 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Large average MG to 7-OH ratios of 30.9 in femoral blood and 32.4 in heart blood were observed compared to average ratios of 14.8 in vitreous humor and 16.9 in urine. Smith et al. (2025) The rise of novel, semi-synthetic 7- hydroxymitragnin e products. NA NA NA NA Letter to editor Began marketing novel semi- synthetic products with varying routes of administration (e.g. sublingual tablets, nasal sprays) containing 14-25 mg. 7-OH-MG per labeled dose, often with brand names alluding to narcotics. These newly marketed products may contain up to 98% 7-OH-MG, together with other kratom alkaloids. Concerningly, some product formulations circumvent first-pass metabolism, increasing bioavailability. Chronic 7-OH product use could result in opioid-like physical dependence and possibly addiction. Scale and severity may be distinct from kratom leaf-based and extract products, which have not produced widespread severe addiction, but rather mild–moderate physical dependence. Currently, 7-OH products contain trace amounts of MG and ‘new’ Page 71 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments chemicals yet to be identified. The safety of these unknown chemicals are unknown Vadiei, Evoy and Grundmann (2025) The Impact of Diverse Kratom Products on Use Patterns, Dependence, and Toxicity NA NA NA NA Although alkaloid content naturally ranges from 2-5% in native leaf material, it can be up to 60% in concentrated extracts. Concentrated kratom products may pose risks not comparable to traditional use, and may require regulatory oversight and clinical evaluation before marketing and therapeutic use. White (2025) Kratom's Use and Impact on Pediatric Populations. MG and 7-OH-MG NA NA Reviewed a case series of 6 neonates exposed prenatally: withdrawal onset ~24 h after birth (jitteriness, irritability, vomiting, poor feeding, crying). Treated successfully with morphine or buprenorphine taper . Review/Letter Poison control (2011–2017, n=1,807 exposures): 10.2% <20 years old. 48 children <13 (42 used kratom only); 137 adolescents 13–19 (80 kratom only). Admission rates after kratom-only exposure: 14.3% (<13 yr), 21.3% (13–19 yr), 27% (≥20 yr). Symptoms: opioid-like (confusion, drowsiness, nausea, vomiting), stimulant-like (agitation, seizures, tremor, tachycardia, hypertension, chest pain, tachypnea). Respiratory depression rare. Children/adolescents may use as a simulant “smart drug” or by athletes for pain/stamina reasons. Page 72 of 128 Publication or Source Short Title or Description Comparators Studied or Mentioned Abuse-related Variables Physical Dependence & Withdrawal Safety Individual Population Comments Wightman and Hu (2025) A Case of 7-OH Mitragynine Use Requiring Inpatient Medically Managed Withdrawal. NA NA NA Patient reported withdrawal symptoms upon cessation of 7-OH use including anxiety, insomnia, rhinorrhea, abdominal discomfort, restlessness, diaphoresis, and chills COWS score peaked at 14 on day 2 38 year old man with history of opioid use disorder reported escalation of use including kratom to 7-OH. Abstinent from opioids then started using kratom at 31 (30 g a day) 3 months before presentation, switched to 7-OH, with escalating use (up to eight 30 mg tablets daily, taking them every 1-2 hours). Patient received buprenorphine and transitioned to residential care. Abbreviations: 7-OH-MG (7-HMG; 7-OH) = 7-hydroxymitragynine; AE(s) = adverse event(s)/adverse effect(s); BBB = blood brain barrier; Cmax = maximum concentration; CNS = central nervous system; COWS = Clinical Opiate Withdrawal Scale; CPP = conditioned place preference; CYP = cytochrome; DOR = delta (δ)- opioid receptor; GI = gastrointestinal; IC50 = half maximal inhibitory concentration; IP = intraperitoneal; Ki = inhibitor constant; IV = intravenous; KOR = kappa (ƙ)- opioid receptor; LLOQ = lower limit of quantitation; MG (MTG) = mitragynine; MGP (MP) = mitragynine pseudoindoxyl; MOR = mu (µ)- opioid receptor; NA = not available; Oxy = oxycodone; P-gp = P-glycoprotein; PK = pharmacokinetic; SC = subcutaneous; SOWS = Subjective Opiate Withdrawal Scale; t1/2 = half life; Tmax = time to maximum concentration. Page 73 of 128 11.2 Appendix 2: Press Release: FDA Takes Steps to Restrict 7-OH Opioid Products Threatening American Consumers Page 74 of 128 Page 75 of 128 11.3 Appendix 3: FDA Report: 7-Hydroxymitragyine (7-OH): An Assessment of the Scientific Data and Toxicological Concerns Around an Emerging Opioid Threat Page 76 of 128 Page 77 of 128 Page 78 of 128 Page 79 of 128 Page 80 of 128 Page 81 of 128 Page 82 of 128 Page 83 of 128 Page 84 of 128 Page 85 of 128 Page 86 of 128 Page 87 of 128 Page 88 of 128 Page 89 of 128 Page 90 of 128 Page 91 of 128 Page 92 of 128 Page 93 of 128 Page 94 of 128 Page 95 of 128 Page 96 of 128 Page 97 of 128 Page 98 of 128 Page 99 of 128 Page 100 of 128 11.4 Appendix 4: FDA Slide Set: Preventing The Next Wave of the Opioid Epidemic: What You Need to Know About 7-OH Page 101 of 128 Page 102 of 128 Page 103 of 128 Page 104 of 128 Page 105 of 128 Page 106 of 128 11.5 Appendix 5: Department of Health and Human Services Press Conference Transcript Measures to Safeguard American Public from Dangerous Opioid 7-OH Participants: HHS Secretary Robert F. Kennedy, Jr. HHS Deputy Secretary Jim O’Neill FDA Commissioner Dr. Marty Makary Melody Woolf (chronic pain survivor). Hubert H. Humphrey Building Auditorium 200 Independence Ave SW Washington, D.C. Tuesday, July 29 at 10:30 AM Eastern Daylight Time. Announcement accessed at https://www.hhs.gov/press-room/hhs-opioid-7oh-press- conference-kennedy.html Page 107 of 128 Page 108 of 128 Page 109 of 128 Page 110 of 128 Page 111 of 128 Page 112 of 128 Page 113 of 128 Page 114 of 128 Page 115 of 128 Page 116 of 128 Page 117 of 128 Page 118 of 128 Page 119 of 128 Page 120 of 128 Page 121 of 128 Page 122 of 128 Page 123 of 128 Page 124 of 128 Page 125 of 128 Page 126 of 128 Page 127 of 128 Page 128 of 128 11.6 Appendix 6: Dr. Martin A. Makary 7-OH Letter to Colleagues