Jublia (efinaconazole)

Efinaconazole, a triazole derivative, is a synthetic azole antifungal agent.

Efinaconazole, a synthetic azole antifungal agent, is a triazole derivative. Like other azole antifungals, efinaconazole presumably exerts its antifungal activity by altering cellular membranes, resulting in increased permeability and growth inhibition. The mechanism of action of efinaconazole may involve inhibition of 14-alpha-demethylase in susceptible fungi, which leads to accumulation of C-14-methylated sterols (e.g., lanosterol) and decreased concentrations of ergosterol in fungal cell membranes.

Depletion of ergosterol affects cell membrane integrity and function and leads to fungal cell death. Antifungal activity of efinaconazole is not affected by the presence of keratin.

Efinaconazole is active against some dermatophytes, including Trichophyton mentagrophytes, T. rubrum, Epidermophyton floccosum, Microsporum canis, and M. gypseum. In vitro, efinaconazole appears to be as active or more active than ciclopirox, itraconazole, and terbinafine against T. mentagrophytes and T. rubrum. Efinaconazole also has in vitro activity against some other fungi, including Candida albicans, Acremonium, Aspergillus, and Scopulariopsis.

There is no evidence to date that T. mentagrophytes or T. rubrum develops resistance to efinaconazole following long-term topical treatment of onychomycosis caused by these dermatophytes, and it has been suggested that there is only a low potential for these fungi to develop resistance to efinaconazole. While the clinical importance is unclear, T. mentagrophytes, T. rubrum, and C. albicans with reduced susceptibility to efinaconazole have been reported in vitro in serial passage resistance studies that used subinhibitory concentrations of the drug.

For the topical treatment of onychomycosis, efinaconazole is commercially available as a 10% solution. The clear colorless to pale yellow solution contains efinaconazole in an alcohol-based vehicle. The topical solution also contains anhydrous citric acid, butylated hydroxytoluene, C12-15 alkyl lactate, cyclomethicone, diiospropyl adipate, disodium edetate, and purified water.

Efinaconazole 10% solution is flammable and should not be stored or used near heat or open flame. (See Topical Administration under Dosage and Administration: Administration.)

Following topical application of efinaconazole 10% solution to toenails in healthy individuals or individuals with severe onychomycosis, low concentrations are absorbed systemically. In vitro studies suggest that efinaconazole has a low binding affinity for keratin and is readily released from keratinized nail plates; this may increase availability of the drug at the site of nail fungal infection and increase penetration through the nail plate. Systemically absorbed efinaconazole undergoes oxidative metabolism via multiple cytochrome P-450 (CYP) isoenzymes, principally 2C19 and 3A4; the major metabolite (H3) is inactive.

In a study in 18 adults with severe onychomycosis involving both great toenails and at least 4 other toenails, efinaconazole topical 10% solution was applied to all 10 toenails and up to 0.5 cm of skin surrounding each toenail once daily for 28 consecutive days. On day 28, mean peak plasma concentrations of efinaconazole were 0.67 ng/mL. Steady state was achieved after about 14 days of once-daily topical application.

Efinaconazole appears to have a long apparent elimination half-life since plasma concentrations of the drug were still detectable in several patients 2 weeks after the last dose. In a study in healthy adults, a plasma half-life of 29.9 hours was reported after 7 days of once-daily topical application to all 10 toenails.

USES: This medication is used to treat toenail infection caused by fungus. It works by stopping the growth of certain types of fungus. Efinaconazole belongs to a class of drugs known as azole antifungals.

Generic name: efinaconazole
Pronunciation: (EF-in-a-KON-a-zole)
Drug class: Topical Antifungals
Therapeutic class: Dermatological

The following indications are listed for Jublia:

• Toenail Onychomycosis

Also known as: Onychomycosis Of Toenail, Tinea Unguium Of Toenail.