Efinaconazole 10% topical solution for the topical treatment of onychomycosis of the toenail

Abstract

Efinaconazole 10% topical solution is a new antifungal therapy for the topical treatment of mild to moderate toenail onychomycosis. In vitro and in vivo data have shown significant antifungal activity against dermatophytes, Candida spp. and nondermatophyte molds, and its mechanism of action is through inhibition of fungal lanosterol 14α-demethylase. In two parallel, double-blind, randomized, controlled, Phase III trials, complete cure rates were 17.8 and 15.2%, respectively, and mycological cure rates were 55.2 and 53.4%, respectively, for efinaconazole 10% topical solution, which were superior to vehicle, with minimal adverse events. This drug profile reviews the most recent basic science and clinical data for efinaconazole in the treatment of toenail onychomycosis.

Keywords:

• efinaconazole
• fungal infection
• Jublia
• nail infection
• onychomycosis
• toenail

Financial & competing interests disclosure

S Lipner is a consultant for Sandoz and R Scher is a consultant, investigator and speaker for multiple companies, including those with antifungal products, and is a consultant and speaker for Valeant. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Key issues

• Efinaconazole 10% solution was US FDA approved in June 2014 for the topical treatment of mild to moderate toenail onychomycosis due to Trichophyton rubrum and Trichophyton mentagrophytes.

• The recommended treatment course is once daily for 48 weeks and no debridement is necessary.

• Its mechanism of action is through inhibition of the ergosterol pathway via 14α-demethylase, with secondary degenerative changes.

• In vitro, efinaconazole has broad-spectrum antifungal activity against dermatophytes, nondermatophyte molds and yeasts, low keratin binding and rapid release from keratin.

• Phase I trials showed that systemic exposure and the potential for drug–drug interactions are remote.

• Since Phase II trials demonstrated that complete and mycological cure rates were superior in the nonoccluded efinaconazole 10% group compared to the efinaconazole 10% semi-occluded group, efinaconazole 5% group and vehicle group, it was chosen to be used in the Phase III trials.

• In two parallel, double-blind, randomized, controlled, Phase III trials, complete cure rates were 17.8 and 15.2%, respectively, and mycological cure rates were 55.2 and 53.4%, respectively, for efinaconazole 10% topical solution, which were superior to vehicle, with minimal adverse events.

Notes