Drug intelligence / Profile preview

abacavir + ethanol

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

**Abacavir + ethanol** is a combination of the nucleoside reverse transcriptase inhibitor abacavir and the alcohol ethanol administered together for study of their pharmacokinetic (PK) interaction. Abacavir is primarily indicated for the treatment of HIV-1 infection as part of combination antiretroviral therapy. Its active metabolite is carbocyclic GTP, which inhibits HIV reverse transcriptase. Both abacavir and ethanol are metabolized by alcohol dehydrogenase, and co-administration results in a significant increase in abacavir plasma exposure (AUC↑41%, Cmax↑15%, half-life↑26%). Ethanol inhibits abacavir’s carboxylate metabolite formation, leading to higher abacavir plasma concentrations. No clinically relevant impact on ethanol PK or safety signals beyond known adverse events of each compound have been identified[1][2]. Abacavir is developed and manufactured by GSK (formerly Glaxo Wellcome)[1][2].

02

Targets

ADH (Alcohol dehydrogenase family)Human immunodeficiency virus type 1 reverse transcriptase

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