Drug intelligence / Profile preview

extended-release naltrexone

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

Overview

Extended-release naltrexone is a long-acting formulation of the opioid antagonist naltrexone, administered as a monthly intramuscular injection. It is FDA-approved for the treatment of both opioid use disorder (OUD) and alcohol use disorder (AUD). The drug works by binding to and blocking mu-opioid receptors in the brain, thereby reducing cravings and preventing the euphoric and sedative effects of opioids and alcohol. Extended-release formulations were developed to address issues with patient noncompliance seen with daily oral dosing. The most widely used product is based on a polylactide glycolide (PLG) polymer microsphere delivery system that allows for sustained release over four weeks[1][2][3][5]. Extended-release naltrexone should only be initiated after patients are fully detoxified from opioids to avoid precipitated withdrawal[2][6]. It is not addictive, does not cause withdrawal symptoms upon discontinuation, and has no abuse potential[1].

Brand names
Vivitrol
Other names
extended-release injectable naltrexoneXR-naltrexoneXR-NTX
02

Targets

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

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