Drug intelligence / Profile preview

ketotifen + olopatadine

Development stage
Preclinical
Lead developer
Sandoz
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Ophthalmic
01

Overview

Ketotifen + olopatadine is a combination of two ophthalmic drugs, ketotifen and olopatadine, both used for the treatment of allergic conjunctivitis and other ocular allergies. Both agents act as dual-action antiallergic medications with antihistamine activity (histamine H1 receptor antagonism) and mast cell stabilization properties. Ketotifen stabilizes mast cells to prevent degranulation and also blocks histamine H1 receptors, reducing symptoms such as itching, redness, and swelling. Olopatadine is a potent selective histamine H1 receptor antagonist that also inhibits the release of histamine from human conjunctival mast cells without causing degranulation. The combination would theoretically provide additive or synergistic effects in controlling allergic eye symptoms by targeting multiple pathways involved in ocular allergy[5][6]. Both drugs are generally well tolerated; common side effects include transient stinging or burning upon instillation and headache[1][5].

02

Targets

HRH1 (Histamine H1 Receptor)

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