Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate

AbstractScope:The purpose of this review is to examine published non-clinical literature on the antihistamine bepotastine besilate, including pharmacokinetic and pharmacologic properties.Methods:Standard literature searches using diverse databases were used to find articles on bepotastine besilate published between 1997 and 2009. Articles primarily described non-clinical data utilized for the development of an oral formulation of bepotastine besilate and were published in Japanese. No publications of non-clinical data for an ophthalmic formulation were found in the database searches.Findings:Bepotastine besilate is a second-generation antihistamine drug possessing selective histamine H1 receptor antagonist activity. Bepotastine has negligible affinity for receptors associated with undesirable adverse effects, including histamine H3, α1‐, α2-, and β-adrenergic, serotonin (5-HT2), muscarinic, and benzodiazepine receptors. Bepotastine possesses additional anti-allergic activity including stabilization of mas...