Drug intelligence / Profile preview

ravuconazole

Development stage
Phase 2
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Ravuconazole is a triazole antifungal agent that acts by inhibiting cytochrome P450 sterol 14α-demethylase (also known as lanosterol 14α-demethylase), an enzyme essential for ergosterol biosynthesis in fungi. Inhibition of this enzyme disrupts the synthesis of ergosterol, a key component of fungal cell membranes, leading to increased membrane permeability and ultimately fungal cell death. It has broad-spectrum activity against various fungi, including Aspergillus spp., Candida spp., and others. Originally developed by Eisai and later investigated by Bristol Myers Squibb, ravuconazole was studied for indications such as aspergillosis, candidiasis, onychomycosis, histoplasmosis, and other mycoses. Despite promising in vitro activity and favorable pharmacokinetics (notably a long half-life), clinical development was discontinued after phase II trials due to strategic reasons rather than safety or efficacy concerns[1][2][3][4][6][7].

Other names
ravuconazolravuconazolumRavuconazole [INN]RAVUCONAZOLE [MI]RAVUCONAZOLE [MART.]RAVUCONAZOLE [WHO-DD]CHEBI:143825
02

Targets

CYP51A1 (Sterol 14α-demethylase)

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