Trade names Kerydin ATC code None CAS Number 174671-46-6 | Routes of
administration Topical Synonyms AN2690 Molar mass 151.93 g/mol | |
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Legal status In general: ℞ (Prescription only) | ||
Tavaborole (AN2690, trade name Kerydin) is a topical antifungal medication for the treatment of onychomycosis, a fungal infection of the nail and nail bed. Tavaborole began its Phase 3 trials in December 2010 and was approved by the US FDA in July 2014. Tavaborole inhibits an essential fungal enzyme, leucyl-tRNA synthetase, that is required for protein synthesis. The inhibition of protein synthesis leads to termination of cell growth and then cell death, eliminating the fungal infection.
Contents
Pharmacokinetics
Tavaborole, when prepared with a 1:1 mixture of ethyl acetate and propylene glycol, has the ability to fully penetrate through the human nail. In studies with cadaver fingernails, a 5% solution of tavaborole penetrated the nail an average of 524.7 mcg/cm2 after two weeks of daily use.
Clinical
Tavaborole is detectable in the blood at a level of 3.54 ng/mL after a single use of 0.2 mL of the 5% solution. Tavaborole has a half-life in the blood of 28.5 hrs, a maximum concentration of 5.17 ng/mL after two weeks of daily use, and takes 8.03 days to reach the maximum concentration.
Therapeutic trials
In clinical trials, tavaborole was more effective than the vehicle (ethyl acetate and propylene glycol) alone in curing onychomycosis. In two studies, fungal infection was eliminated using tavaborole in 6.5% of the cases vs. 0.5% using the vehicle alone, and 27.5% vs. 14.6% using the vehicle alone.
Adverse effects
Application site exfoliation, erythema (rash), and irritation are all possible side effects, though they occur in less than 5% of the patents tested.
Commercial
Originally developed by Anacor, it is now marketed in the United States by Novartis subsidiary Sandoz. Anacor was paid US$65 million and also entered into a profit sharing scheme for future sales. A 10mL bottle of a 5% solution of Tavaborole will cost the patient without insurance about $1,356.