Drug intelligence / Profile preview

naltrexone + bupropion SR

Development stage
Unknown
Lead developer
Orexigen Therapeutics, Inc
Modality
Small Molecules
Administration
Intramuscular, Oral
01

Overview

This combination pharmacotherapy consists of extended-release injectable naltrexone and oral extended-release bupropion, specifically investigated by the National Institute on Drug Abuse (NIDA) for the treatment of methamphetamine use disorder. Naltrexone is a mu-opioid receptor antagonist that reduces the euphoric effects of substance use, while bupropion is a norepinephrine-dopamine reuptake inhibitor (NDRI) that addresses withdrawal symptoms and dysphoria. The combination was evaluated in the ADAPT-2 trial, demonstrating significant efficacy in increasing response rates among adults with moderate to severe methamphetamine use disorder compared to placebo. There is currently no FDA-approved medication for methamphetamine use disorder, making this combination a significant investigational treatment option.

Other names
naltrexone and bupropion SRNX/BUP
02

Targets

NET (Norepinephrine Transporter)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)DAT (Dopamine plasma membrane transport protein)OCT2 (Organic cation transporter 2)

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