vapitadine

Vapitadine (R-129160) is a selective, non-sedating small molecule antihistamine that acts as a potent antagonist of the histamine H1 receptor (Ki = 19 nM). Originally discovered by Johnson & Johnson and subsequently licensed to Stiefel Laboratories (later acquired by GSK) and Barrier Therapeutics, the drug was investigated for the treatment of allergic skin reactions, including chronic idiopathic urticaria and pruritus associated with atopic dermatitis. A defining characteristic of vapitadine is its lack of blood-brain barrier penetration, which prevents the sedative effects common in first-generation antihistamines. Although it reached Phase II clinical trials and demonstrated efficacy in reducing itch symptoms, development appears to have been discontinued as no further progress has been reported since the completion of those trials.

Brand names

Hivenyl

Other names

vapitadine dihydrochlorideR129160R-129160R 129160