Samidorphan

Opioid Antagonist — NERVOUS SYSTEM

Key facts

Samidorphan is an onp drug in the Opioid Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2021. Its mechanism of action is classified as Opioid Antagonists. DrugCentral lists 3 molecular targets, including OPRM1, OPRK1 and OPRD1. Recorded indications include Bipolar I disorder and Schizophrenia.

• Approval status: onp (first approved 2021 by the FDA).
• Drug class: Opioid Antagonist.
• Mechanism of action: Opioid Antagonists.
• Molecular targets: OPRM1, OPRK1 and OPRD1 (3 listed in DrugCentral).
• Indications: Bipolar I disorder and Schizophrenia.
• ATC code: N05AH53 (Diazepines, oxazepines, thiazepines and oxepines).
• Molecular formula: C21H26N2O4; molecular weight 370.45 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Bipolar I disorder
• Schizophrenia

Mechanism & targets

• Mechanism of action (MoA): Opioid Antagonists
• Established pharmacologic class: Opioid Antagonist

Molecular targets (3)

Target	Gene	Action	Activity
Mu-type opioid receptor	OPRM1	antagonist	Ki 10.28
Kappa-type opioid receptor	OPRK1	partial agonist	Ki 9.64
Delta-type opioid receptor	OPRD1	partial agonist	Ki 8.59

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2021-05-28	FDA	—	ALKERMES INC

ATC classification

ATC code	Therapeutic hierarchy
N05AH53	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines

Chemical structure

• Molecular formula: C₂₁H₂₆N₂O₄
• Molecular weight: 370.45 g/mol
• CAS number: 852626-89-2
• InChIKey: RYIDHLJADOKWFM-UHFFFAOYSA-N
• PubChem CID: 11667832

C1CC1CN2CCC34CC(=O)CCC3(C2CC5=C4C(=C(C=C5)C(=O)N)O)O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Samidorphan used for?

DrugCentral lists the following indications for Samidorphan: Bipolar I disorder and Schizophrenia.

How does Samidorphan work?

Samidorphan is classified as Opioid Antagonists; its molecular targets in DrugCentral include OPRM1 (antagonist), OPRK1 (partial agonist) and OPRD1 (partial agonist).

When was Samidorphan first approved?

Samidorphan was first approved by the FDA in 2021.

What drug class does Samidorphan belong to?

Samidorphan is in the Opioid Antagonist class.

What is the chemical formula of Samidorphan?

Samidorphan has the molecular formula C21H26N2O4 and a molecular weight of 370.45 g/mol.

Sources

• DrugCentral drug card 5460 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2105749 — compound record and bioactivity
• PubChem CID 11667832 — chemical identifiers
• DrugBank DB12543 — drug record
• FDA UNII 7W2581Z5L8 — substance identity
• DailyMed: FDA labels for Samidorphan — current prescribing information (label search)
• UniProt P35372 (OPRM1) — target protein
• UniProt P41145 (OPRK1) — target protein
• UniProt P41143 (OPRD1) — target protein

How this page is built: methodology · editorial policy & corrections.