Drug intelligence / Profile preview

fluconazole

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Fluconazole is a synthetic triazole antifungal agent used to treat and prevent a wide range of fungal infections. It acts by inhibiting the fungal cytochrome P450 enzyme lanosterol 14-alpha-demethylase, which is essential for converting lanosterol to ergosterol—a key component of the fungal cell membrane. This disruption impairs cell membrane formation and function, leading to inhibition of fungal growth or death. Fluconazole is effective against most Candida species (except some resistant strains), Cryptococcus neoformans, dermatophytes, and certain other fungi. It is commonly prescribed for vaginal candidiasis (yeast infection), oropharyngeal and esophageal candidiasis (thrush), systemic Candida infections including candidemia and pneumonia, cryptococcal meningitis, urinary tract infections caused by Candida species, peritonitis due to Candida infection, as well as prophylaxis in immunocompromised patients such as those undergoing bone marrow transplantation or with advanced HIV/AIDS[1][2][3][6][8]. Fluconazole can be administered orally (tablet or suspension) or intravenously[3][4][7].

Brand names
Diflucan
Other names
氟康唑fluconazolfluconazolumFCZ
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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