Drug intelligence / Profile preview

nevirapine + fluconazole

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**Nevirapine + fluconazole** is a combination of two small-molecule pharmaceutical drugs: **nevirapine**, a non-nucleoside reverse transcriptase inhibitor (NNRTI) used primarily in antiretroviral therapy for HIV-1 infection, and **fluconazole**, a triazole antifungal agent used to treat and prevent fungal infections. When co-administered, fluconazole inhibits cytochrome P450 enzymes (notably CYP3A4 and CYP2B6), which results in reduced hepatic metabolism of nevirapine, leading to a significant increase in nevirapine plasma concentrations. While fluconazole’s effect on nevirapine efficacy is pharmacokinetic rather than pharmacodynamic, this interaction increases the risk of nevirapine-related adverse events, particularly hepatotoxicity and, less commonly, rash. This combination is sometimes used in the context of HIV/AIDS, especially where antifungal prophylaxis or treatment is required simultaneously with antiretroviral therapy[1][2][3][4].

02

Targets

Gag-Pol (HIV-1 gag-pol polyprotein)Human immunodeficiency virus type 1 reverse transcriptaseCYP2B6 (Cytochrome P450 2B6)CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)

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