Examining the benefits of the boron-based mechanism of action and physicochemical properties of tavaborole in the treatment of onychomycosis

Bryan Markinson, Mahmoud Ghannoum, Tate Winter, Anthony Rycerz, Fernando Rock, Aditya K. Gupta

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

Onychomycosis is a fungal infection of the nail primarily caused by the dermatophytes Trichophyton rubrum and Trichophyton mentagrophytes. The topical-based treatment of onychomycosis remains a challenge because of the difficulty associated with penetrating the dense, protective structure of the keratinized nail plate. Tavaborole is a novel smallmolecule antifungal agent recently approved in the United States for the topical treatment of toenail onychomycosis. The low molecular weight, slight water solubility, and boron chemistry of tavaborole maximize nail penetration after topical application, allowing for effective targeting of the infection in the nail bed. The efficacy of tavaborole is associated with its novel mechanism of action, whereby it inhibits the fungal leucyltRNA synthetase (LeuRS) enzyme. Because LeuRS is an essential component in fungal protein synthesis, inhibition of LeuRS ultimately leads to fungal cell death. Tavaborole is the first boron-based antifungal medication approved for the treatment of mild-tomoderate onychomycosis and presents patients with a new topical option. Previously, ciclopirox and efinaconazole were the only approved topical treatments for onychomycosis. This article details the properties that are at the core of the clinical benefits associated with tavaborole.

Original languageEnglish
Pages (from-to)12-19
Number of pages8
JournalJournal of the American Podiatric Medical Association
Volume108
Issue number1
DOIs
StatePublished - Jan 2018

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