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embeconazole

Development stage: Discontinued
Lead developer: Daiichi Sankyo
Modality: Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration: Oral

Overview

Embeconazole (CS-758 or R-120758) is a triazole antifungal agent developed by Daiichi Sankyo. It acts as a potent inhibitor of lanosterol 14 alpha-demethylase (fungal CYP51A1), an enzyme essential for ergosterol biosynthesis in fungi. By inhibiting this enzyme, embeconazole disrupts fungal cell membrane formation, leading to antifungal effects. The drug demonstrated strong in vitro and in vivo activity against various yeasts and molds, including Candida and Aspergillus species[1][2][3]. Embeconazole was investigated primarily for the treatment of mycoses but its clinical development was discontinued after early-phase trials[6].

Other names: embeconazoletriazole antifungal agent

Targets

CYP51A1 (Sterol 14α-demethylase)

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