Drug intelligence / Profile preview

disulfiram + efavirenz

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two small molecule drugs: **disulfiram**, an aldehyde dehydrogenase inhibitor used as a deterrent in the treatment of alcohol dependence, and **efavirenz**, a non-nucleoside reverse transcriptase inhibitor used as part of antiretroviral therapy for HIV infection. Disulfiram works by irreversibly inhibiting aldehyde dehydrogenase, leading to accumulation of acetaldehyde when alcohol is consumed, causing unpleasant effects that discourage drinking[1][3]. Efavirenz inhibits HIV reverse transcriptase by binding to an allosteric site on the enzyme, preventing viral replication[2]. When co-administered, efavirenz can increase the inhibitory effect of disulfiram on aldehyde dehydrogenase due to induction of CYP3A4-mediated metabolism that increases levels of the active metabolite responsible for ALDH inhibition[1][4]. This combination may be considered in patients with co-occurring HIV infection and alcohol use disorder.

Brand names
Stocrin
Other names
tetraethylthiuram disulfideNNRTI
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)ALDH1A1 (Aldehyde dehydrogenase 1 family member A1)

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