title: Mechanism of action of efinaconazole, a novel triazole antifungal agent.
abstract: 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.
authors: Central Research Laboratories, Kaken Pharmaceutical Co, Ltd, Kyoto, Japan. tatsumi_yoshiyuki@kaken.co.jp
authors: Yoshiyuki
authors: Y
authors: Tatsumi
authors: Maria
authors: M
authors: Nagashima
authors: Toshiyuki
authors: T
authors: Shibanushi
authors: Atsushi
authors: A
authors: Iwata
authors: Yumi
authors: Y
authors: Kangawa
authors: Fumie
authors: F
authors: Inui
authors: William J Jo
authors: WJ
authors: Siu
authors: Radhakrishnan
authors: R
authors: Pillai
authors: Yayoi
authors: Y
authors: Nishiyama
mesh_terms: D058888:14-alpha Demethylase Inhibitors / Q000494:pharmacology*; D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism / Q000648:ultrastructure; D004305:Dose-Response Relationship, Drug; D004875:Ergosterol / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D025301:Hyphae / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism / Q000648:ultrastructure; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D013261:Sterols / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D014230:Triazoles / Q000494:pharmacology*; D014249:Trichophyton / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism / Q000648:ultrastructure
chemical_list: D058888:14-alpha Demethylase Inhibitors; D000935:Antifungal Agents; D013261:Sterols; D014230:Triazoles; C431707:efinaconazole; D004875:Ergosterol