Last reviewed 2026-04-22 · How we verify

Bepotastine besilate formulation

Bepotastine besilate is a selective H1-receptor antagonist that blocks histamine signaling to reduce allergic symptoms.

Bepotastine besilate is a selective H1-receptor antagonist that blocks histamine signaling to reduce allergic symptoms. Used for Allergic conjunctivitis.

At a glance

Mechanism of action

Bepotastine competitively antagonizes H1 histamine receptors on mast cells and other immune cells, preventing histamine-mediated allergic responses. It is formulated as an ophthalmic solution for topical ocular administration, where it rapidly penetrates the eye to provide local anti-allergic effects with minimal systemic absorption.

Approved indications

• Allergic conjunctivitis

Common side effects

• Ocular irritation
• Headache
• Taste perversion
• Conjunctival hyperemia

Key clinical trials

• Bepotastine Besilate-corticosteroid Nasal Spray Combination Compared to Placebo, Bepotastine Besilate Nasal Spray, and Corticosteroid Nasal Spray in the Treatment of Patients With Seasonal Allergic Rhinitis (PHASE2)
• Bepreve vs. Alrex in Subjects With Moderate to Severe Allergic Conjunctivitis (PHASE4)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Bepotastine besilate formulation CI brief — competitive landscape report
• Bepotastine besilate formulation updates RSS · CI watch RSS
• Bausch & Lomb Incorporated portfolio CI