Oteseconazole

Oteseconazole (CAS No. 1340593-59-0) is a potent and selective tetrazole CYP51 (lanosterol 14α-demethylase) inhibitor, whose core bioactivity is to inhibit the growth of Candida and other fungi. By targeting and binding fungal CYP51, it blocks ergosterol biosynthesis and disrupts cell membrane integrity, and it shows high selectivity for human cytochrome P450 enzymes, reducing the risk of drug-drug interactions. IC?? data are well defined: the IC?? for human CYP3A4 is 65 μM, which is significantly higher than that of imidazole and triazole drugs. Its MIC is pathogen-specific: the MIC?? values against Candida albicans (SC5314, CPCC400616), Candida tropicalis, Candida parapsilosis, Candida glabrata, Candida krusei, Cryptococcus neoformans, etc. are all ≤0.00625~0.1 μg/mL, it shows no inhibitory activity against Aspergillus fumigatus (MIC>64 μg/mL), and it remains active against fluconazole-resistant Candida. Common application concentrations: in vitro antimicrobial tests use gradient concentrations of 0.00625~0.1 μg/mL (for Candida spp.). Clinically effective therapeutic concentrations correspond to the approved dosing for its indication, for the prevention of recurrent vulvovaginal candidiasis (RVVC), maintaining plasma concentrations above the MIC values for Candida via oral administration. The high selectivity achieved through structural optimization significantly reduces the risk of drug-drug interactions in clinical use and confers good tolerability.

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