Ketoconazole is a broad-spectrum triazole antifungal agent that has activity against C. albicans, C. krusei, C. tropicalis, C. glabrata, C. parapsilosis, C. neoformans, and A. fumigatus strains (IC50s = 0.031-8 ?g/ml).1 It inhibits the fungal cytochrome P450 (CYP) isoform CYP51, also known as lanosterol 14α-demethylase, which arrests ergosterol biosynthesis at the fungal membrane. Ketoconazole also inhibits human CYP3A4 (IC50 = 0.54 ?M). Formulations containing ketoconazole have been used in the treatment of fungal infections.
1.Dilmaghanian, S., Gerber, J.G., Filler, D.G., et al.Enantioselectivity of inhibition of cytochrome P450 3A4 (CYP3A4) by ketoconazole: Testosterone and methadone as substratesChirality16(2)79-85(2004)