Samidorphan
Samidorphan is an opioid receptor antagonist with mixed opioid receptor activity, developed as an adjunct to olanzapine for the treatment of bipolar I disorder and as a component of the combination product for major depressive disorder. By blocking mu-opioid receptors, it attenuates the weight gain and metabolic effects associated with olanzapine therapy without diminishing its antipsychotic efficacy. It is co-formulated with olanzapine in the fixed-dose combination product Lybalvi.
Peso Molecular
370,4000 g/mol
LogP
1,10
TPSA
104,00 Ų
Regra dos 5 de Lipinski
Aprovado
Áreas Terapêuticas
Mecanismo de Ação
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Estrutura 2D
Cite this structure
Embed this structure
SMILES
NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCC(=O)C3
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
Molecular Formula
C21H26N2O4
HBD / HBA
3 / 5
Ligações Rotacionáveis
3
Átomos Pesados
27
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Perguntas frequentes
Samidorphan is an opioid receptor antagonist with mixed opioid receptor activity, developed as an adjunct to olanzapine for the treatment of bipolar I disorder and as a component of the combination product for major depressive disorder. By blocking mu-opioid receptors, it attenuates the weight gain and metabolic effects associated with olanzapine therapy without diminishing its antipsychotic efficacy. It is co-formulated with olanzapine in the fixed-dose combination product Lybalvi.
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Yes, Samidorphan is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL426084. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 11667832. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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