TY - JOUR
T1 - Examining the benefits of the boron-based mechanism of action and physicochemical properties of tavaborole in the treatment of onychomycosis
AU - Markinson, Bryan
AU - Ghannoum, Mahmoud
AU - Winter, Tate
AU - Rycerz, Anthony
AU - Rock, Fernando
AU - Gupta, Aditya K.
N1 - Publisher Copyright:
© 2018, American Podiatric Medical Association. All rights reserved.
PY - 2018/1
Y1 - 2018/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85053899338&partnerID=8YFLogxK
U2 - 10.7547/16-154
DO - 10.7547/16-154
M3 - Article
C2 - 29547036
AN - SCOPUS:85053899338
SN - 8750-7315
VL - 108
SP - 12
EP - 19
JO - Journal of the American Podiatric Medical Association
JF - Journal of the American Podiatric Medical Association
IS - 1
ER -