Central Research Laboratories, Kaken Pharmaceutical Co, Ltd, Kyoto, Japan.
Antimicrob Agents Chemother. 2013 May;57(5):2405-9. doi: 10.1128/AAC.02063-12. Epub 2013 Mar 4.
The mechanism of action of efinaconazole, a new triazole antifungal, was investigated with Trichophyton mentagrophytes and Candida albicans. Efinaconazole dose-dependently decreased ergosterol production and accumulated 4,4-dimethylsterols and 4α-methylsterols at concentrations below its MICs. Efinaconazole induced morphological and ultrastructural changes in T. mentagrophytes hyphae that became more prominent with increasing drug concentrations. In conclusion, the primary mechanism of action of efinaconazole is blockage of ergosterol biosynthesis, presumably through sterol 14α-demethylase inhibition, leading to secondary degenerative changes.
新型三唑类抗真菌药依氟康唑的作用机制通过须毛癣菌和白色念珠菌进行了研究。依氟康唑剂量依赖性地降低麦角固醇的产生，并在低于 MIC 的浓度下积累 4,4-二甲基固醇和 4α-甲基固醇。依氟康唑诱导须毛癣菌菌丝的形态和超微结构发生变化，随着药物浓度的增加，变化更加明显。总之，依氟康唑的主要作用机制是阻断麦角固醇生物合成，可能通过抑制甾醇 14α-去甲基酶，导致次级退行性变化。
