Nalmefene

Opioid Antagonist — NERVOUS SYSTEM

Key facts

Nalmefene is an ofp drug in the Opioid Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1995. Its mechanism of action is classified as Opioid Antagonists. DrugCentral lists 6 molecular targets, including OPRK1, Oprm1 and OPRM1. Recorded indications include Alcoholism, Opiate-Induced Respiratory Depression and Poisoning by opiate analgesic drug.

• Approval status: ofp (first approved 1995 by the FDA).
• Drug class: Opioid Antagonist.
• Mechanism of action: Opioid Antagonists.
• Molecular targets: OPRK1, Oprm1, OPRM1 and OPRD1 (6 listed in DrugCentral).
• Indications: Alcoholism, Opiate-Induced Respiratory Depression and Poisoning by opiate analgesic drug.
• ATC code: N07BB05 (Drugs used in alcohol dependence).
• Molecular formula: C21H25NO3; molecular weight 339.44 g/mol.

Indications & contraindications

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

Indications (3)

• Alcoholism
• Opiate-Induced Respiratory Depression
• Poisoning by opiate analgesic drug

Mechanism & targets

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

Molecular targets (6)

Target	Gene	Action	Activity
Kappa-type opioid receptor	OPRK1	antagonist	Ki 9.92
Mu-type opioid receptor	Oprm1	unknown	Ki 9.54
Mu-type opioid receptor	OPRM1	antagonist	Kd 9.53
Delta-type opioid receptor	OPRD1	antagonist	Kd 9.04
Kappa-type opioid receptor	OPRK1	unknown	Ki 8.70
Delta-type opioid receptor	Oprd1	unknown	Ki 8.47

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2019-08-01	PMDA	—	OTSUKA PHARMACEUTICAL CO., LTD.
1995-04-17	FDA	—	EUROHLTH INTL SARL

ATC classification

ATC code	Therapeutic hierarchy
N07BB05	NERVOUS SYSTEM › OTHER NERVOUS SYSTEM DRUGS › DRUGS USED IN ADDICTIVE DISORDERS › Drugs used in alcohol dependence

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Drug withdrawal syndrome	237.0
Coma	202.9
Drug interaction	114.3
Respiratory depression	88.8
Bradypnoea	66.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Nalmefene is on its molecule page.

• Molecular formula: C₂₁H₂₅NO₃
• Molecular weight: 339.44 g/mol
• CAS number: 55096-26-9
• InChIKey: WJBLNOPPDWQMCH-MBPVOVBZSA-N
• PubChem CID: 5284594

OC1=C2O[C@H]3C(=C)CC[C@@]4(O)[C@H]5CC(C=C1)=C2[C@@]34CCN5CC1CC1

Frequently asked questions

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

What is Nalmefene used for?

DrugCentral lists the following indications for Nalmefene: Alcoholism, Opiate-Induced Respiratory Depression and Poisoning by opiate analgesic drug.

How does Nalmefene work?

Nalmefene is classified as Opioid Antagonists; its molecular targets in DrugCentral include OPRK1 (antagonist), Oprm1, OPRM1 (antagonist) and OPRD1 (antagonist).

When was Nalmefene first approved?

Nalmefene was first approved by the FDA in 1995.

What drug class does Nalmefene belong to?

Nalmefene is in the Opioid Antagonist class.

What is the chemical formula of Nalmefene?

Nalmefene has the molecular formula C21H25NO3 and a molecular weight of 339.44 g/mol.

Sources

• DrugCentral drug card 1876 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201152 — compound record and bioactivity
• PubChem CID 5284594 — chemical identifiers
• DrugBank DB06230 — drug record
• FDA UNII TOV02TDP9I — substance identity
• DailyMed: FDA labels for Nalmefene — current prescribing information (label search)
• UniProt P41145 (OPRK1) — target protein
• UniProt P35372 (OPRM1) — target protein
• UniProt P41143 (OPRD1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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