Oteseconazole

Oteseconazole is an azole metalloenzyme inhibitor that targets fungal CYP51. CYP51, also known as 14α demethylase, participates in the formation of ergosterol, a compound that plays a vital role in the integrity of cell membranes. By binding and inhibiting CYP51, oteseconazole is active against most microorganisms associated with recurrent vulvovaginal candidiasis (RVVC). Oteseconazole has demonstrated activity against Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, Candida tropicalis, Candida lusitaniae and Candida dubliniensis.

Unlike previous-generation azole antifungals, oteseconazole has a high selectivity for CYP51 and little interaction with human cytochrome P450s. This is possible thanks to the tetrazole moiety in oteseconazole that increases target selectivity. In contrast with oteseconazole, other antifungals with imidazole or triazole moieties, such as ketoconazole or fluconazole, have a high number of drug-drug interactions due to their interaction with human CYPs.

The use of oteseconazole is contraindicated in females of reproductive potential due to its embryo-fetal toxicity risks. This drug was approved by the FDA on April 26, 2022.

Oteseconazole is an azole antifungal indicated to reduce the incidence of recurrent vulvovaginal candidiasis (RVVC) in females with a history of RVVC who are not of reproductive potential.