Drug intelligence / Profile preview

dapivirine + miconazole

Development stage
Unknown
Lead developer
Population Council
Modality
Small Molecules
Administration
Vaginal
01

Overview

This is a **combination of dapivirine**, a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for HIV prevention, and **miconazole**, an imidazole antifungal usually used to treat vulvovaginal candidiasis. Both drugs are delivered vaginally. Dapivirine acts by inhibiting HIV-1 reverse transcriptase, thereby preventing viral replication, while miconazole inhibits the synthesis of ergosterol, an essential component of fungal cell membranes, leading to fungal cell death. Studies show that co-administration alters the pharmacokinetic profiles of both drugs, mainly due to **drug-drug interactions at the level of CYP enzymes**. Miconazole inhibits CYP1A1 and CYP3A4, decreasing the metabolism of dapivirine and increasing its systemic concentration. Dapivirine has modest effects on the metabolism of miconazole. The combination has been evaluated in a clinical trial for the prevention of HIV and treatment of vulvovaginal candidiasis in women[1][2][3][4].

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP51A1 (Sterol 14α-demethylase)CYP1A1 (Cytochrome P450 1A1)CYP3A4 (Cytochrome P450 3A4)

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