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Compound

Samidorphan

Original Wikipedia articleen.wikipedia.org/wiki/Samidorphan revision used (24 October 2026)

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Overview

Samidorphan (INN (International Nonproprietary Name), USAN (United States Adopted Name)) is an opioid antagonist that in the form of olanzapine/samidorphan (sold as Lybalvi) is used in the treatment of schizophrenia and bipolar disorder. Samidorphan reduces the weight gain associated with olanzapine. Samidorphan is taken by mouth.[1–5] WP

Samidorphan was under development as a standalone medication for various indications but has been discontinued. Buprenorphine/samidorphan for the treatment of major depressive disorder was rejected by the US Food and Drug Administration (FDA) due to insufficient evidence of effectiveness, but remains in preregistration as of September 2021. Development of baclofen/samidorphan has also been discontinued.[6][7][8] WP

Risks and side effects

Side effects

Side effects of samidorphan include somnolence and gastrointestinal disturbances among others.[1] WP

Pharmacology

Pharmacodynamics

Samidorphan acts primarily as an antagonist or very weak partial agonist of the μ-opioid receptor (MOR) and to a lesser extent as a partial agonist of the κ-opioid receptor (KOR) and δ-opioid receptor (DOR). In accordance with this profile, samidorphan has been observed to produce some side effects that are potentially consistent with activation of the KOR such as somnolence, sedation, dizziness, and hallucinations in some patients in clinical trials.[1][9][10][11] WP

Pharmacokinetics

The elimination half-life of samidorphan is 7 to 9 hours.[1][12] WP

Chemistry

Formula
C21H26N2O4 PC
CAS number
852626-89-2 PC
Molar mass (g/mol)
370.4 PC
IUPAC name (computed by PubChem)
(1R,9R,10S)-17-(cyclopropylmethyl)-3,10-dihydroxy-13-oxo-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-triene-4-carboxamide PC
SMILES
C1CC1CN2CC[C@]34CC(=O)CC[C@]3([C@H]2CC5=C4C(=C(C=C5)C(=O)N)O)O PC
InChIKey
RYIDHLJADOKWFM-MAODMQOUSA-N PC
PubChem CID
11667832
IUPAC name
17-(Cyclopropylmethyl)-4,14-dihydroxy-6-oxomorphinan-3-carboxamide WP

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

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Sources

  1. Journal / agency Chaudhary AM, Khan MF, Dhillon SS, Naveed S. A Review of Samidorphan: A Novel Opioid Antagonist. Cureus. July 2019. doi:10.7759/cureus.5139 · PMID 31523568 · PMC6741386
  2. Journal / agency LYBALVI: Highlight of Prescribing Information
  3. Journal / agency Olanzapine/samidorphan - Alkermes plc
  4. Journal / agency Citrome L, Graham C, Simmons A, Jiang Y, Todtenkopf MS, Silverman B, DiPetrillo L, Cummings H, Sun L, McDonnell D. An Evidence-Based Review of OLZ/SAM for Treatment of Adults with Schizophrenia or Bipolar I Disorder. Neuropsychiatric Disease and Treatment. 2021. doi:10.2147/NDT.S313840 · PMID 34526769 · PMC8437420
  5. Journal / agency Paik J. Olanzapine/Samidorphan: First Approval. Drugs. August 2021. doi:10.1007/s40265-021-01568-0 · PMID 34304374
  6. Journal / agency Samidorphan
  7. Journal / agency Buprenorphine/samidorphan - Alkermes
  8. Journal / agency Baclofen/samidorphan
  9. Other Linda P. Dwoskin. Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse. 29 January 2014
  10. Journal / agency Wentland MP, Lou R, Lu Q, Bu Y, Denhardt C, Jin J, Ganorkar R, VanAlstine MA, Guo C, Cohen DJ, Bidlack JM. Syntheses of novel high affinity ligands for opioid receptors. Bioorganic & Medicinal Chemistry Letters. April 2009. doi:10.1016/j.bmcl.2009.02.078 · PMID 19282177 · PMC2791460
  11. Journal / agency McElroy SL, Guerdjikova AI, Blom TJ, Crow SJ, Memisoglu A, Silverman BL, Ehrich EW. A placebo-controlled pilot study of the novel opioid receptor antagonist ALKS-33 in binge eating disorder. The International Journal of Eating Disorders. April 2013. doi:10.1002/eat.22114 · PMID 23381803
  12. Journal / agency Turncliff R, DiPetrillo L, Silverman B, Ehrich E. Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers. Clinical Therapeutics. February 2015. doi:10.1016/j.clinthera.2014.10.001 · PMID 25456560

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.