Samidorphan

Samidorphan
Clinical data
Other namesALKS-33; RDC-0313; 3-Carboxamido-4-hydroxynaltrexone
Routes of
administration		By mouth
Pharmacokinetic data
Elimination half-life7–9 hours[1][2]
Identifiers
IUPAC name
  • 17-(Cyclopropylmethyl)-4,14-dihydroxy-6-oxomorphinan-3-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H26N2O4
Molar mass370.449 g·mol−1
3D model (JSmol)
SMILES
  • c1cc(c(c2c1C[C@@H]3[C@]4([C@]2(CCN3CC5CC5)CC(=O)CC4)O)O)C(=O)N
InChI
  • InChI=1S/C21H26N2O4/c22-19(26)15-4-3-13-9-16-21(27)6-5-14(24)10-20(21,17(13)18(15)25)7-8-23(16)11-12-1-2-12/h3-4,12,16,25,27H,1-2,5-11H2,(H2,22,26)/t16-,20-,21-/m1/s1
  • Key:RYIDHLJADOKWFM-MAODMQOUSA-N

Samidorphan (INNTooltip International Nonproprietary Name, USANTooltip 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.[1][3][4] Samidorphan reduces the weight gain associated with olanzapine.[5][6] Samidorphan is taken by mouth.[1][3]

Samidorphan was under development as a standalone medication for various indications but has been discontinued.[7] 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.[8] Development of baclofen/samidorphan has also been discontinued.[9]

  1. ^ a b c Chaudhary AM, Khan MF, Dhillon SS, Naveed S (July 2019). "A Review of Samidorphan: A Novel Opioid Antagonist". Cureus. 11 (7): e5139. doi:10.7759/cureus.5139. PMC 6741386. PMID 31523568.
  2. ^ Turncliff R, DiPetrillo L, Silverman B, Ehrich E (February 2015). "Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers". Clinical Therapeutics. 37 (2): 338–348. doi:10.1016/j.clinthera.2014.10.001. PMID 25456560.
  3. ^ a b "LYBALVI: Highlight of Prescribing Information" (PDF). U.S. Food and Drug Administration. Archived from the original (PDF) on June 1, 2021.
  4. ^ "Olanzapine/samidorphan - Alkermes plc". Adis Insight. Springer Nature Switzerland AG.
  5. ^ Citrome L, Graham C, Simmons A, Jiang Y, Todtenkopf MS, Silverman B, et al. (2021). "An Evidence-Based Review of OLZ/SAM for Treatment of Adults with Schizophrenia or Bipolar I Disorder". Neuropsychiatric Disease and Treatment. 17: 2885–2904. doi:10.2147/NDT.S313840. PMC 8437420. PMID 34526769.
  6. ^ Paik J (August 2021). "Olanzapine/Samidorphan: First Approval". Drugs. 81 (12): 1431–1436. doi:10.1007/s40265-021-01568-0. PMID 34304374. S2CID 236215923.
  7. ^ "Samidorphan". Adis Insight. Springer Nature Switzerland AG.
  8. ^ "Buprenorphine/samidorphan - Alkermes". Adis Insight. Springer Nature Switzerland AG.
  9. ^ "Baclofen/samidorphan". Adis Insight. Springer Nature Switzerland AG.
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