Literature DB >> 23459486

Mechanism of action of efinaconazole, a novel triazole antifungal agent.

Yoshiyuki Tatsumi1, Maria Nagashima, Toshiyuki Shibanushi, Atsushi Iwata, Yumi Kangawa, Fumie Inui, William J Jo Siu, Radhakrishnan Pillai, Yayoi Nishiyama.   

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.

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Year:  2013        PMID： 23459486      PMCID： PMC3632939          DOI： 10.1128/AAC.02063-12

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  18 in total

1.  In vitro antifungal activity of KP-103, a novel triazole derivative, and its therapeutic efficacy against experimental plantar tinea pedis and cutaneous candidiasis in guinea pigs.

Authors:  Y Tatsumi; M Yokoo; T Arika; H Yamaguchi
Journal:  Antimicrob Agents Chemother       Date:  2001-05       Impact factor: 5.191

2.  Degenerative changes in fungi after itraconazole treatment.

Authors:  M Borgers; M A Van de Ven
Journal:  Rev Infect Dis       Date:  1987 Jan-Feb

3.  Impact of pH on the antifungal susceptibility of vaginal Candida albicans.

Authors:  Wei Liu; Xu Zhang; Zhaohui Liu; Xin Luo
Journal:  Int J Gynaecol Obstet       Date:  2011-06-21       Impact factor: 3.561

4.  Effect of the antimycotic drug naftifine on growth of and sterol biosynthesis in Candida albicans.

Authors:  N S Ryder; G Seidl; P F Troke
Journal:  Antimicrob Agents Chemother       Date:  1984-04       Impact factor: 5.191

5.  The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis.

Authors:  Hugo Vanden Bossche; Jannie Ausma; Hilde Bohets; Karen Vermuyten; Gustaaf Willemsens; Patrick Marichal; Lieven Meerpoel; Frank Odds; Marcel Borgers
Journal:  Antimicrob Agents Chemother       Date:  2004-09       Impact factor: 5.191

6.  Multiple functions for sterols in Saccharomyces cerevisiae.

Authors:  R J Rodriguez; C Low; C D Bottema; L W Parks
Journal:  Biochim Biophys Acta       Date:  1985-12-04

Review 7.  History of the development of azole derivatives.

Authors:  J A Maertens
Journal:  Clin Microbiol Infect       Date:  2004-03       Impact factor: 8.067

8.  Effect of miconazole and clotrimazole on K+ release and inhibition of ergosterol biosynthesis in Trichophyton mentagrophytes and related ultrastructural observations.

Authors:  E M Scott; S P Gorman; J S Millership; L R Wright
Journal:  J Antimicrob Chemother       Date:  1986-04       Impact factor: 5.790

9.  Comparison of miconazole- and ketoconazole-induced release of K+ from Candida species.

Authors:  W H Beggs
Journal:  J Antimicrob Chemother       Date:  1983-04       Impact factor: 5.790

10.  The effect of bifonazole on the structure of Trichophyton mentagrophytes.

Authors:  M Osumi; N Yamada; Y Yamada; H Yamaguchi
Journal:  Dermatologica       Date:  1984
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  14 in total

1.  Morphological Effect of the New Antifungal Agent ME1111 on Hyphal Growth of Trichophyton mentagrophytes, Determined by Scanning and Transmission Electron Microscopy.

Authors:  Yayoi Nishiyama; Sho Takahata; Shigeru Abe
Journal:  Antimicrob Agents Chemother       Date:  2016-12-27       Impact factor: 5.191

2.  Effects of two 6-quinolinyl chalcones on the integrity of plasma membrane of Paracoccidioides brasiliensis.

Authors:  Nívea P de Sá; Patrícia S Cisalpino; Luciana C Tavares; Leandro Espíndola; Beatriz M Borelli; Paulo Js Barbeira; Gabriele de Matos Cardoso Perdigão; Elaine M Souza-Fagundes; Carlos A Rosa; Moacir G Pizzolatti; Susana Johann
Journal:  J Antibiot (Tokyo)       Date:  2017-01-11       Impact factor: 2.649

3.  In Vitro Activities of Luliconazole, Lanoconazole, and Efinaconazole Compared with Those of Five Antifungal Drugs against Melanized Fungi and Relatives.

Authors:  Gholam Reza Shokoohi; Hamid Badali; Hossein Mirhendi; Saham Ansari; Ali Rezaei-Matehkolaei; Bahram Ahmadi; Afsane Vaezi; Mohamed Mahdi Alshahni; Koichi Makimura
Journal:  Antimicrob Agents Chemother       Date:  2017-10-24       Impact factor: 5.191

4.  Effect of Topical Antifungal Luliconazole on Hyphal Morphology of Trichophyton mentagrophytes Grown on in vitro Onychomycosis Model.

Authors:  Yayoi Nishiyama; Mari Maeda; Tsuyoshi Yamada
Journal:  Mycopathologia       Date:  2022-09-03       Impact factor: 3.785

5.  Efinaconazole: first global approval.

Authors:  Trina Patel; Sohita Dhillon
Journal:  Drugs       Date:  2013-11       Impact factor: 9.546

Review 6.  Efinaconazole in the treatment of onychomycosis.

Authors:  Shari R Lipner; Richard K Scher
Journal:  Infect Drug Resist       Date:  2015-06-01       Impact factor: 4.003

7.  Effects of Streptococcus sanguinis Bacteriocin on Cell Surface Hydrophobicity, Membrane Permeability, and Ultrastructure of Candida Thallus.

Authors:  Shengli Ma; Yingnan Zhao; Xue Xia; Xue Dong; Wenyu Ge; Hui Li
Journal:  Biomed Res Int       Date:  2015-04-29       Impact factor: 3.411

Review 8.  Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis.

Authors:  Liliana Scorzoni; Ana C A de Paula E Silva; Caroline M Marcos; Patrícia A Assato; Wanessa C M A de Melo; Haroldo C de Oliveira; Caroline B Costa-Orlandi; Maria J S Mendes-Giannini; Ana M Fusco-Almeida
Journal:  Front Microbiol       Date:  2017-01-23       Impact factor: 5.640

Review 9.  The Dermatologist's Approach to Onychomycosis.

Authors:  Jenna N Queller; Neal Bhatia
Journal:  J Fungi (Basel)       Date:  2015-08-19

10.  An Assessment of In Vitro Antifungal Activities of Efinaconazole and Itraconazole against Common Non-Dermatophyte Fungi Causing Onychomycosis.

Authors:  Ananya Tupaki-Sreepurna; Bhavna T Jishnu; Vijayakishore Thanneru; Savitri Sharma; Anjana Gopi; Murugan Sundaram; Anupma Jyoti Kindo
Journal:  J Fungi (Basel)       Date:  2017-05-05
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