Mechanism of Action of Efinaconazole, a Novel Triazole Antifungal Agent-Reference-Cited by-同舟云学术

Mechanism of Action of Efinaconazole, a Novel Triazole Antifungal Agent

Published:2013-05 Issue:5 Volume:57 Page:2405-2409
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Tatsumi Yoshiyuki¹,Nagashima Maria¹,Shibanushi Toshiyuki²,Iwata Atsushi¹,Kangawa Yumi²,Inui Fumie¹,Siu William J. Jo³,Pillai Radhakrishnan³,Nishiyama Yayoi⁴

Affiliation:

1. Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Kyoto, Japan

2. Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Fujieda, Shizuoka, Japan

3. Dow Pharmaceutical Sciences, a division of Valeant Pharmaceuticals North America LLC, Petaluma, California, USA

4. Teikyo University Institute of Medical Mycology, Tokyo, Japan

Abstract

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.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.02063-12

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