Drug intelligence / Profile preview

naltrexone (Alkermes, 391ce2)

Development stage
Approved
Lead developer
Alkermes
Modality
Small Molecules
Administration
Intmuscular
01

Overview

Extended-release naltrexone injection, 380 mg (marketed under the brand name Vivitrol) is an FDA-approved intramuscular depot formulation of naltrexone. It is formulated as microspheres using a biodegradable polylactide-co-glycolide (PLG) polymer matrix, which gradually releases naltrexone over approximately 4 weeks following a single gluteal intramuscular injection. Naltrexone is a small molecule opioid antagonist that acts as a competitive antagonist at mu-opioid receptors in the brain, blocking the euphoric and reinforcing effects of both exogenous opioids and endogenous endorphins. This formulation is indicated for the treatment of alcohol dependence in patients who can abstain from alcohol in an outpatient setting, and for the prevention of relapse to opioid dependence following opioid detoxification. By providing sustained therapeutic blood levels for a month, it addresses the compliance challenges associated with daily oral naltrexone therapy.

Brand names
VivitrolVivitrex
Other names
extended-release naltrexoneextended-release naltrexone injection, 380 mgnaltrexone for extended-release injectable suspension
02

Targets

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

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