Bepotastine is effective against allergic conjunctivitis in research

Key Points

Cincinnati-Bepotastine besilate ophthalmic solution 1.0% (Bepreve, ISTA Pharmaceuticals) has been shown to be effective in reducing ocular itching, the hallmark symptom of allergic conjunctivitis, but it also seems to have secondary benefits in decreasing nasal symptoms associated with ocular allergies, said Thomas T. Macejko, MD.

"Bepotastine besilate is unique because it is active against many different parts of the inflammatory and allergy response," said Dr. Macejko, who is in private practice in Cincinnati. "It also has a strong safety record in Japan as an oral agent, was well tolerated in the U.S. clinical trials, and produces a reduction in other non-ocular allergy symptoms as a secondary benefit."

Under review

Bepotastine was approved in Japan as an oral tablet to treat allergic rhinitis in July 2000 and pruritus accompanying urticaria and certain skin diseases in January 2002. The medication is marketed by Mitsubishi Tanabe Pharma Company Ltd. (formerly Tanabe Seiyaku Co. Ltd.) under the brand name Talion. In 2006, ISTA Pharmaceuticals acquired the North American rights to develop, manufacture, and market bepotastine for ophthalmic use under a licensing agreement with Senju. ISTA Pharmaceuticals' new drug application for bepotastine was accepted for review by the FDA in late January of this year.

Selective antagonist

"Bepotastine besilate has a broad attack through different mechanisms to diminish the allergic response," Dr. Macejko said. It is a selective antagonist of the histamine 1 receptor on mast cells and eosinophils and also inhibits migration of eosinophils into inflamed tissues, which reduces chemosis and redness, he said. The drop also stabilizes mast cells, inhibits platelet activating factor, and interferes with production of interleukin-5, a key inflammatory cytokine, Dr. Macejko added.

He also commented on a study of bepotastine in which he was not an investigator. In that single-site clinical trial, bepotastine appeared to provide rapid relief from ocular itching and rhinorrhea associated with allergic conjunctivitis. An abstract on the clinical benefit for reduction of ocular itching associated with allergic conjunctivitis provided by bepotastine 1.0% was presented at the most recent American Academy of Ophthalmology (AAO) annual meeting.

The double-masked, randomized, placebo-controlled, 7-week clinical trial enrolled 72 subjects who were assigned to receive either bepotastine (n = 36) or placebo (n = 36). The subjects underwent an initial CAC screening with allergen titration to induce bilateral ocular itching and conjunctival redness grades ≥ 2 using a standardized 0 to 4 scale. Allergen confirmation was performed at a second study visit. About 4 weeks later, a CAC test assessing efficacy for 8-hour duration of action was conducted after bilateral instillation of one drop of drug or placebo. Two weeks after the 8-hour duration of action CAC test, an onset of action CAC test was performed 15 minutes after dosing. Bepotastine was found to be clinically and statistically superior to placebo both for a rapid onset of action and with duration of action of at least 8 hours, he said.