Drug intelligence / Profile preview

bupropion + naltrexone

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

Overview

Bupropion + naltrexone is a combination therapy being investigated by researchers at the University of Minnesota for the treatment of tobacco use disorder (smoking cessation). This combination utilizes the complementary mechanisms of bupropion, a norepinephrine and dopamine reuptake inhibitor (NDRI) and nicotinic acetylcholine receptor antagonist, and naltrexone, an opioid receptor antagonist that also modulates nicotinic receptor activity. By targeting the brain's reward system and reducing the reinforcing effects of nicotine, the combination aims to improve abstinence rates compared to monotherapy. A Phase II clinical trial (NCT00419731) conducted by the University of Minnesota demonstrated that the combination of bupropion (300 mg/day) and naltrexone (50 mg/day) significantly increased 7-day point-prevalence abstinence rates compared to bupropion alone.

Other names
bupropion/naltrexonenaltrexone/bupropionbupropion + naltrexonenaltrexone + bupropion
02

Targets

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

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