Tavaborole (tavaborole)

Tavaborole, a boron-containing compound, is an oxaborole antifungal agent.

Tavaborole is an oxaborole antifungal agent. Oxaboroles are boron-containing molecules with antifungal activity. Integration of boron into the cyclic structure of a molecule allows for greater stability, greater physiologic availability at the required site of action, and effective target binding capacity and selectivity.

The mechanism of action of tavaborole against susceptible fungi involves inhibition of fungal protein synthesis by inhibition of an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS). Tavaborole inhibits the editing domain of leucyl-tRNA synthetase and exhibits good relative selectivity for this fungal enzyme. Antifungal activity of tavaborole is not affected by the presence of keratin.

Tavaborole is active against some dermatophytes, including Trichophyton mentagrophytes and T. rubrum. The drug also has antifungal activity in vitro against Candida albicans. There is no evidence to date that T. mentagrophytes or T. rubrum develops resistance to tavaborole following long-term topical treatment of onychomycosis caused by these dermatophytes.

For the topical treatment of onychomycosis, tavaborole is commercially available as a 5% solution. Each mL of the clear, colorless solution contains 43.5 mg of tavaborole in an alcohol-based vehicle. The topical solution also contains edetate calcium disodium and propylene glycol.

Tavaborole 5% 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 tavaborole 5% solution to toenails, the drug penetrates the nail plate and low concentrations are absorbed systemically. In a study in 24 adults with distal subungual onychomycosis involving at least 4 toenails (including at least 1 great toenail), tavaborole topical 5% solution was applied to all 10 toenails and up to 2 mm of skin surrounding each toenail once daily (total of 0.2 mL once daily) for 14 consecutive days. Mean peak plasma concentration of tavaborole was 3.54 ng/mL (range 0.618-10.2 ng/mL) after a single dose.

After 14 consecutive days of once-daily topical administration, mean peak plasma concentration of the drug was 5.17 ng/mL (range 1.51-12.8 ng/mL) and median time to peak plasma concentration was 8.03 hours (range 0.47-24 hours). Steady state was achieved after 14 days of once-daily topical application. At steady state, the mean terminal plasma half-life of tavaborole was 28.5 hours based on data available from 10 individuals.

Systemically absorbed tavaborole undergoes extensive metabolism and is eliminated principally by the kidneys.

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

Generic name: tavaborole
Pronunciation: (TA-va-BOR-ole)
Drug class: Topical Antifungals
Therapeutic class: Dermatological

The following indications are listed for Tavaborole:

• Toenail Onychomycosis

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