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J. Fungi 2017, 3(4), 58; https://doi.org/10.3390/jof3040058

Fungicidal Activity in the Presence of Keratin as an Important Factor Contributing to In Vivo Efficacy: A Comparison of Efinaconazole, Tavaborole, and Ciclopirox

Pharmacology Department, Drug Research Center, Kaken Pharmaceutical Co., Ltd. 14, Shinomiya, Minamigawara-cho, Yamashina-ku, Kyoto 607-8042, Japan
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Received: 12 September 2017 / Revised: 12 October 2017 / Accepted: 17 October 2017 / Published: 19 October 2017
(This article belongs to the Special Issue Antifungal Susceptibility Testing)
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Abstract

Use of oral antifungals in the treatment of onychomycosis is commonplace; but their use can be limited by safety and patient concerns. Due to their broader safety margins, topical antifungals (efinaconazole, tavaborole, and ciclopirox) are a useful option in the treatment of mild-to-moderate onychomycosis in the USA, but their antifungal activity has yet to be directly compared. This study aims to identify important factors contributing to in vivo efficacies of the three topical antifungals. Minimum inhibitory concentrations (MICs) were determined by Clinical and Laboratory Standards Institute (CLSI) M38-A2 broth microdilution. The MIC90 values of efinaconazole, tavaborole, and ciclopirox for T. rubrum were 0.0078, 8.0, and 0.50 μg/mL, respectively. The MIC90 values for T. mentagrophytes were 0.016, 8.0, and 0.50 μg/mL, respectively. Efinaconazole showed potent fungicidal activity in keratin-containing medium, whereas tavaborole was fungistatic, and ciclopirox not active. In the guinea pig model of onychomycosis, the therapeutic efficacy of efinaconazole was superior to those of tavaborole and ciclopirox. This study suggests that not only fungistatic activity (MIC), but also fungicidal activity in the presence of keratin, is an important factor contributing to the in vivo efficacy of topical antifungal drugs against onychomycosis. View Full-Text
Keywords: onychomycosis; topical antifungal; drug effect; keratin; fungicidal activity onychomycosis; topical antifungal; drug effect; keratin; fungicidal activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Tachibana, H.; Kumagai, N.; Tatsumi, Y. Fungicidal Activity in the Presence of Keratin as an Important Factor Contributing to In Vivo Efficacy: A Comparison of Efinaconazole, Tavaborole, and Ciclopirox. J. Fungi 2017, 3, 58.

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