Drug intelligence / Profile preview

brimonidine + ketotifen

Development stage
Phase 3
Lead developer
Bausch & Lomb
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Brimonidine + ketotifen is a fixed-dose combination ophthalmic solution developed for the treatment of allergic conjunctivitis. Brimonidine is a highly selective alpha-2 adrenergic receptor agonist that acts primarily by reducing intraocular pressure through decreased aqueous humor production and increased uveoscleral outflow. It also causes vasoconstriction, which can reduce ocular redness[6][4]. Ketotifen is an antihistamine and mast cell stabilizer that works by blocking histamine H1 receptors and preventing the release of mediators involved in allergic responses, thereby relieving itching and other symptoms associated with allergic conjunctivitis[2][8]. The combination aims to provide both rapid relief from itching (via antihistaminic action) and reduction in ocular redness (via vasoconstriction), offering a dual mechanism for symptomatic management of eye allergies[3][8]. The product has been evaluated in multiple clinical trials, including phase 3 and phase 4 studies, for safety and efficacy in patients with allergic conjunctivitis[1][5].

Other names
brimonidine tartrate + ketotifen fumarate
02

Targets

ADRA2A (α2A)HRH1 (Histamine H1 Receptor)

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