Drug intelligence / Profile preview

metronidazole + fluconazole

Development stage
Unknown
Lead developer
University of Washington
Modality
Small Molecules
Administration
Oral
01

Overview

metronidazole + fluconazole is a combination regimen evaluated by the University of Washington for the prevention of vaginal infections in high-risk populations. Metronidazole is a nitroimidazole antibiotic that acts as a prodrug; it is reduced in anaerobic bacteria to form reactive intermediates that cause DNA strand breakage and inhibit DNA synthesis. Fluconazole is a triazole antifungal that selectively inhibits the fungal enzyme lanosterol 14-alpha-demethylase (CYP51A1), thereby blocking the conversion of lanosterol to ergosterol, an essential component of the fungal cell membrane. This specific combination was studied as a monthly oral prophylaxis (2 grams of metronidazole and 150 mg of fluconazole) in a Phase 3 trial in Mombasa, Kenya, where it demonstrated a significant reduction in the incidence of bacterial vaginosis and an increase in healthy Lactobacillus colonization among HIV-negative female sex workers.

Other names
metronizadole-University of Washington-vaginal infectionMonthly Metronidazole and FluconazoleMonthly Metronidazole and Fluconazole for Vaginal Infection Prevention
02

Targets

CYP51A1 (Sterol 14α-demethylase)

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