Drug intelligence / Profile preview

disulfiram + naltrexone

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral
01

Overview

Disulfiram + naltrexone is a combination therapy used in the management of alcohol dependence. Disulfiram acts by inhibiting aldehyde dehydrogenase, leading to accumulation of acetaldehyde when alcohol is consumed, which results in unpleasant physiological reactions (such as flushing, nausea, and hypotension) that deter drinking. It also inhibits dopamine-β-hydroxylase. Naltrexone is an opioid receptor antagonist that blocks the effects of endogenous opioids involved in the rewarding effects of alcohol consumption. Both drugs are FDA-approved for treating alcoholism individually; their combination has been studied for potential additive or synergistic benefits but evidence suggests only modest advantage over monotherapy and no clear superiority for the combination[1][2][3]. The use of both agents together may increase risk for hepatotoxicity and should be monitored carefully[5].

02

Targets

ALDH2 (Mitochondrial Aldehyde Dehydrogenase)DOR (Opioid Receptor Delta 1)DBH (Dopamine beta-hydroxylase)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)ALDH1A1 (Aldehyde dehydrogenase 1 family member A1)

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