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voriconazole
- Development stage
- Approved
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Voriconazole is a second-generation, broad-spectrum triazole antifungal agent used to treat serious fungal infections, particularly in immunocompromised patients. It is effective against invasive aspergillosis, candidemia (including esophageal and deep tissue Candida infections), coccidioidomycosis, histoplasmosis, penicilliosis, and infections caused by Scedosporium and Fusarium species. Voriconazole works by inhibiting the fungal cytochrome P450 enzyme 14-alpha-lanosterol demethylase (CYP51), which blocks the conversion of lanosterol to ergosterol—a critical component of the fungal cell membrane—thereby disrupting membrane synthesis and function. This action limits fungal growth (fungistatic effect) and allows the host immune system to clear infection[1][3][4][5]. Developed originally by Pfizer as Vfend, it is available in oral tablet, oral suspension, and intravenous formulations.
- Brand names
- Vfend
- Other names
- 伏立康唑
02
Targets
CYP51A1 (Sterol 14α-demethylase)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2C19 (Cytochrome P450 2C19)CYP3A4 (Cytochrome P450 3A4)
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