Bepotastine besilate ophthalmic solution 1.5% for alleviating nasal symptoms in patients with allergic conjunctivitis

Abstract

Background: Bepotastine besilate ophthalmic solution (BBOS) 1.5% is a topical antihistamine for the treatment of ocular itching associated with allergic conjunctivitis (AC). Allergic rhinitis and AC are common comorbid conditions. We explored the efficacy of BBOS 1.5% in alleviating nasal symptoms in an integrated analysis of two Phase III conjunctival allergen challenge (CAC) studies and a Phase IV environmental allergen study.

Methods: In the Phase III trials, a CAC was performed 15 minutes, 8 hours, and 16 hours following ocular instillation of BBOS 1.5% (n=78) or placebo (n=79), and subjects evaluated nasal symptoms. In the environmental study, subjects instilled BBOS 1.5% (n=123) or placebo (n=122) twice daily and nasal symptoms were evaluated over 2 weeks.

Results: In the Phase III trials, BBOS 1.5% had reduced CAC-induced nasal congestion and pruritus at 15 minutes and 8 hours postdosing and rhinorrhea and a non-ocular composite-symptom score (sum of nasal scores plus ear or palate pruritus) at all time points postdosing (all P≤0.01 vs placebo). In the Phase IV environmental study, BBOS 1.5% reduced sneezing and nasal pruritus over 2 weeks and median number of days to improvement of nasal pruritus and total nasal symptom score (sum for rhinorrhea, sneezing, nasal pruritus, and nasal congestion; P≤0.04 vs placebo). Additionally, investigator-reported improvement in overall ocular (pruritus, hyperemia, tearing) and nasal symptoms was greater with BBOS 1.5% vs placebo (P≤0.03).

Conclusion: Results of these exploratory analyses indicate that topical ocular BBOS 1.5% reduced nasal symptoms, supporting its use for alleviating rhinitis symptoms associated with AC.

Keywords: allergic rhinitis; antihistamine; bepotastine besilate; conjunctival allergen challenge; conjunctivitis; nasal symptoms.

Figure 1

Phase III conjunctival allergen challenge (CAC) study design. Notes: CACs were administered 15 minutes (onset of action), 16 hours and 8 hours (duration of action) after treatment instillation and nasal symptoms were measured at 7, 15, and 20 minutes post-CAC. The study also included a BBOS 1% arm, the results of which are not reported here. Abbreviations: BBOS, bepotastine besilate ophthalmic solution; TAI, test-agent instillation.

Figure 2

Phase IV environmental allergen study design. Notes: During the study period, subjects instilled BBOS 1.5% (n=123) or placebo (n=122) and recorded their nasal symptoms twice-daily. At visit 3 (day 7±1), subjects were contacted by phone for compliance and adverse-event assessments. Safety assessments were also conducted at visit 4 (day 14±2). Abbreviation: BBOS, bepotastine besilate ophthalmic solution.

Figure 3

Mean reflective sneezing scores by day and time (ITT population). Notes: Reflective assessment of sneezing was recorded on a 4-point scale twice daily (morning and evening) during baseline assessment and the 2-week treatment period. Baseline value represents averaged responses of the last seven predose sneezing assessments collected at visit 2 (day 0) and twice daily during the 7-day screening period (ie, during the last 3 days of the screening period). *P≤0.05 vs placebo (analysis of covariance). Abbreviations: ITT, intent to treat; BBOS, bepotastine besilate ophthalmic solution.