Bioactivity | Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2]. | ||||||||||||
Invitro | Voriconazole has great activity against S. apiospermum and C. neoformans with the MICs of 0.5 μg/mL and 0.125–0.25 μg/mL, respectively[1].Voriconazole inhibits the cytochrome P450 (CYP)-dependent enzyme 14-alpha-sterol demethylase, thereby disrupting the cell membrane and halting fungal growth[2]. | ||||||||||||
In Vivo | Voriconazole (5-20 mg/kg; p.o. for 21 days) prolongs survival in a dose-dependent fashion. Voriconazole (40 mg/kg/day) decreases the fungal burden in the lungs[3]. Animal Model: | ||||||||||||
Name | Voriconazole | ||||||||||||
CAS | 137234-62-9 | ||||||||||||
Formula | C16H14F3N5O | ||||||||||||
Molar Mass | 349.31 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Nickie D Greer. Voriconazole: the newest triazole antifungal agent.Proc (Bayl Univ Med Cent). 2003 Apr;16(2):241-8. [2]. Lesley J Scott, et al. Voriconazole : a review of its use in the management of invasive fungal infections.Drugs. 2007;67(2):269-98. [3]. A M Sugar,et al. Efficacy of voriconazole in treatment of murine pulmonary blastomycosis.Antimicrob Agents Chemother. 2001 Feb;45(2):601-4. |