Drug intelligence / Profile preview

tavaborole

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Topical
01

Overview

Tavaborole is a novel, boron-based small molecule antifungal agent used topically for the treatment of onychomycosis, a fungal infection of the toenail and nail bed caused primarily by *Trichophyton rubrum* and *Trichophyton mentagrophytes*. Its mechanism of action is unique among antifungals; it inhibits fungal protein synthesis by selectively binding to and inhibiting cytosolic leucyl-tRNA synthetase (LeuRS), an enzyme essential for charging tRNA with leucine during protein translation. This inhibition disrupts fungal cell growth and leads to cell death. Tavaborole demonstrates high specificity for the fungal enzyme over its human counterpart, contributing to its safety profile. It was approved by the FDA in July 2014 and is marketed under the brand name Kerydin.

Brand names
Kerydin
Other names
5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole
02

Targets

LeuRS (Fungal cytoplasmic leucyl-tRNA synthetase (LeuRS) editing domain)

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