Oteseconazole is an azole antifungal used to prevent recurrent vulvovaginal candidiasis in females who are not of reproductive potential. 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. Oteseconazole inhibits the enzyme lanosterol 14-alpha demethylase. Lanosterol 14-alpha demethylase is the enzyme that catalyzes the synthesis of 4,4'-dimethyl cholesta-8,14,24-triene-3-beta-ol from lanosterol. With this enzyme inhibited ergosterol synthesis cannot occur which causes a significant low concentration of ergosterol in the fungal cell. Ergosterol is essential in maintaining membrane integrity in fungi. Without ergosterol, the fungus cell cannot synthesize membranes thereby increasing fluidity and preventing growth of new cells. This leads to cell lysis which causes it to collapse and die.Because of its ability to bind and inhibit CYP51, oteseconazole is active against most microorganisms associated with recurrent vulvovaginal candidiasis (RVVC). Besides blocking the formation of ergosterol, oteseconazole also promotes the accumulation of 14-methylated sterols that lead to fungal cell death.

Oteseconazole Pathway References