Bepotastine Besilate Ophthalmic Solution 1.5% Produces Strong Clinical Benefit for Ocular Itching Immediately Following Dosing in the Conjunctival Allergen Challenge (CAC) Model of Allergic Conjunctivitis

RATIONALE: To establish the effectiveness of bepotastine besilate ophthalmic solution (BBOS) 1.5%, a dual acting histamine H1 receptor antagonist approved by the United States FDA for treatment of ocular itching associated with allergic conjunctivitis, compared to placebo in reducing baseline ocular itching scores for severely allergic subjects in a CAC clinical model of allergic conjunctivitis. METHODS: Ocular itching was scored as a primary endpoint using a 0-4 unit grading scale. A key inclusion criterion in both CAC studies was an itching score of at least 2.0 units in both eyes for a majority of time points at screening. Pooled data from the 2 double-masked, randomized, placebo-controlled, CAC, clinical trials were evaluated post hoc for itching response of subjects with severe allergic reactions to a CAC (i.e., ≥2 itching scores of at least 3.0 units at screening). Eligible subjects were assigned randomly to either BBOS 1.5% or placebo. RESULTS: In the per-protocol population, strong clinical effectiveness (p<0.01) in eyes of severely allergic subjects, defined as a minimum of a 2.0 unit improvement over baseline screening values, was found for BBOS 1.5% (84%) compared to placebo (22%) for reduced ocular itching by 15 minutes post-dosing. For a 3.0 unit improvement in a CAC 15 minutes after dosing, BBOS 1.5% (48%) was also superior to placebo (3%; p<0.01). CONCLUSIONS: BBOS 1.5% was strongly more effective than placebo after ophthalmic dosing in reducing ocular itching as determined from pooled data for severely allergic subjects in 2 CAC clinical studies.