Drug intelligence / Profile preview

tioconazole

Development stage
Approved
Lead developer
Pfizer Laboratories
Modality
Small Molecules
Administration
Topical, Intravaginal
01

Overview

Tioconazole is a broad-spectrum imidazole antifungal agent primarily used to treat fungal and yeast infections. It is most commonly indicated for vulvovaginal candidiasis (vaginal yeast infections), but topical formulations are also used for dermatophyte infections such as ringworm (tinea corporis), jock itch (tinea cruris), athlete's foot (tinea pedis), tinea versicolor ("sun fungus"), and cutaneous candidiasis. Tioconazole acts by inhibiting 14-alpha demethylase, a cytochrome P-450 enzyme involved in converting lanosterol to ergosterol—an essential component of the fungal cell membrane. This inhibition disrupts ergosterol synthesis, increasing cellular permeability and leading to cell death. In addition to its antifungal activity against Candida species and other pathogenic yeasts and dermatophytes, tioconazole exhibits antibacterial effects on certain Gram-positive cocci bacteria[1][5][6]. It is available over-the-counter in various countries as single-dose vaginal ointments or topical creams.

Brand names
Monistat Simple TherapyVagistatVagistat-1Vagistat1Vagistat 1TrosydGyno-Trosyd
Other names
TioconazolTioconazolum
02

Targets

CYP51A1 (Sterol 14α-demethylase)

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