Integrated phase III trials of bepotastine besilate ophthalmic solution 1.5% for ocular itching associated with allergic conjunctivitis

Eye Care Associates of Greater Cincinnati, Inc., Mason, Ohio, USA.
Allergy and Asthma Proceedings (Impact Factor: 3.06). 05/2012; 33(3):265-74. DOI: 10.2500/aap.2012.33.3570
Source: PubMed


Allergic conjunctivitis is a clinical reaction to environmental allergens and is manifested by ocular itching caused by IgE-induced mast cell degranulation. Bepotastine besilate is a selective H(1)-antagonist with mast cell stabilizing properties. This report examines the reduction of ocular itching integrated from two conjunctival allergen challenge (CAC) clinical trials comparing bepotastine besilate ophthalmic solution (BBOS) 1.5% to placebo in subjects with a history of allergic conjunctivitis. Two phase III, double-masked, placebo-controlled, parallel-group, CAC clinical trials evaluated BBOS 1.5% versus placebo to reduce ocular itching. Eligible subjects were randomly assigned 1:1 to either BBOS 1.5% (n = 78) or placebo (n = 79). Ocular itching was graded by subjects using a standardized scale (0–4 U). Adverse events and ophthalmic clinical findings were recorded for safety. BBOS 1.5% was superior to placebo for reducing CAC-induced ocular itching (p < 0.0001) as early as 3 minutes post-CAC and for at least 8 hours after dosing. Post hoc analyses examining several populations also showed a significant improvement (p < 0.0001) for subjects with more severe itching response at screening and for the proportion of subjects with complete or nearly complete resolution of CAC-induced itching, both outcomes supporting the clinical benefit of BBOS 1.5%. Adverse events were generally transient and mild. BBOS 1.5% is safe and effective in the treatment of ocular itching associated with allergic conjunctivitis within 3 minutes of a CAC and with a sustained duration of action of at least 8 hours. ( numbers: NCT00424398 and NCT00586664).

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    ABSTRACT: Allergic conjunctivitis (AC) affects an estimated 20% of the population in the Western world, with a large fraction suffering due to seasonal or perennial allergen exposures. Bepotastine besilate ophthalmic solution (BBOS) 1.5%, a dual-acting histamine(H1)receptor antagonist and mast cell stabilizer, is indicated for itching associated with AC. This study was designed to evaluate the efficacy and safety of BBOS 1.5% for reducing ocular itching associated with AC in subjects enrolled in a natural exposure trial. Eligible subjects in a multicenter, double-masked, randomized, parallel-group, placebo-controlled, naturalexposure clinical trial were randomly assigned to either BBOS 1.5% or placebo eyedrops on a 1;1 basis and instilled 1 drop of the test agent into both eyes twice daily for 2 weeks. The mean change from baseline in instantaneous and reflective ocular itching scores at the end of 2 weeks of treatment were evaluated based on subject-assessed severity of instantaneous andreflective itching. Subject-reported adverse events (AEs) were also recorded for safety. Treatment with BBOS 1.5% significantly reduced instantaneous and reflective ocular itching scores from baseline compared with placebo over the 2-week study period (p = 0.007 and p = 0.005, respectively). BBOS 1.5% was well tolerated, and AEs were generally transient and mild. This clinical study indicates BBOS 1.5% effectively and safely treated ocular itching in a natural exposure allergy study and is auseful treatment option for the management of ocular itching associated with AC. ( identifier number: NCT01174823.).
    Allergy and Asthma Proceedings 03/2013; 34(3). DOI:10.2500/aap.2013.34.3671 · 3.06 Impact Factor
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    ABSTRACT: The focus of this review is to provide a logical paradigm for the diagnosis and treatment of ocular allergies, with a focus on seasonal allergic conjunctivitis (SAC) and perennial allergic conjunctivitis (PAC). Several classes of topical medications are currently available for the management of ocular allergies, including: lubricating agents, vasoconstrictors, antihistamines, mast cell stabilizers, and topical corticosteroids. SAC and PAC make up the vast majority of ocular allergy cases. A proactive approach to these diseases, anticipating the regional spring and fall allergen spikes, is needed for optimally managing these disorders. A multifaceted treatment regimen comprising patient education, lifestyle modification, and topical medications (such as antihistamines and/or mast cell stabilizers and corticosteroids) may be required in order to manage ocular allergies effectively. The appropriate treatment paradigm is based on the severity of the patients' signs and symptoms. For moderate-to-severe cases, especially chronic vernal keratoconjunctivitis, atopic keratoconjunctivitis, and giant papillary conjunctivitis, comanagement with an ophthalmologist is recommended.
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    ABSTRACT: Introduction: Bepotastine besilate 1.5% is a newly approved second-generation topical antihistamine indicated for the pruritus associated with allergic conjunctivitis. In Japan, the oral formulation is approved to manage pruritus associated with allergic rhinitis and urticaria. Areas covered: Bepotastine is a piperidine derivative that antagonizes H1 receptors with high selectivity. It has been labeled a dual-acting or multiple-acting antiallergic medication, because it inhibits histamine at H1 receptors and stabilizes mast cells to prevent histamine release. Bepotastine may also have other immunoactive properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4) and platelet-activating factor (PAF). Human clinical trials demonstrate the efficacy and safety of systemic and ophthalmic bepotastine for pruritus relief, limited penetration across the blood-brain-barrier and kinetics suitable for twice-daily administration. Expert opinion: Bepotastine besilate 1.5% ophthalmic solution is a safe and effective treatment option for allergic conjunctivitis associated pruritus. Side-effect profile is similar to other ocular antihistamine agents. Additional comparative-effectiveness studies would further advance its clinical use. Oral bepotastine is a safe and effective treatment option approved in Japan for allergic rhinitis, urticaria and pruritus associated with skin diseases.
    Expert Opinion on Pharmacotherapy 11/2013; 14(18). DOI:10.1517/14656566.2013.849242 · 3.53 Impact Factor
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