Samidorphan

Samidorphan
Clinical data
Other namesALKS-33; RDC-0313; 3-Carboxamido-4-hydroxynaltrexone
Routes of
administration		Oral
Pharmacokinetic data
Elimination half-life7–9 hours[1][2]
Identifiers
  • 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)
  • c1cc(c(c2c1C[C@@H]3[C@]4([C@]2(CCN3CC5CC5)CC(=O)CC4)O)O)C(=O)N
  • 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) (developmental code names ALKS-33, RDC-0313) is an opioid antagonist that in the form of olanzapine/samidorphan (brand name 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 Food and Drug Administration 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.
  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.