Drug intelligence / Profile preview

nalmefene

Development stage
Approved
Lead developer
Lundbeck
Modality
Small Molecules
Administration
Oral, Intranasal, Intravenous, Intramuscular, Subcutaneous
01

Overview

Nalmefene is an opioid receptor antagonist used primarily for the treatment of opioid overdose and alcohol dependence. It acts as an antagonist at mu-opioid and delta-opioid receptors and as a partial agonist at the kappa-opioid receptor. By blocking these receptors in the brain's reward system, nalmefene reduces the rewarding effects of opioids and alcohol. This mechanism helps reverse life-threatening symptoms of opioid overdose (such as respiratory depression) and decreases alcohol consumption in individuals with alcohol dependence. Nalmefene has a longer duration of action than naloxone and does not induce tolerance or physical dependence[1][2][5][8]. It can be administered orally, intranasally, or by injection.

Brand names
Revex
Other names
nalmefene
02

Targets

DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)KOR (Kappa opioid receptor)

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