Drug intelligence / Profile preview

ketotifen

Development stage
Approved
Lead developer
Sandoz
Modality
Small Molecules
Administration
Oral, Ophthalmic
01

Overview

Ketotifen is an antihistamine and mast cell stabilizer used to treat allergic conditions such as conjunctivitis (allergic pinkeye), asthma, urticaria (hives), atopic dermatitis (eczema), and systemic mast cell diseases like mastocytosis and mast cell activation syndrome. Available in both oral and ophthalmic forms, it reduces the frequency and severity of asthma symptoms when taken daily with other antiasthmatic medications but is not effective for acute attacks. Ketotifen acts primarily as a non-competitive antagonist of the histamine H1 receptor—blocking histamine-mediated reactions such as itching and swelling—and stabilizes mast cells to inhibit the release of inflammatory mediators including histamine, leukotrienes, prostaglandins, tryptase, and platelet-activating factor. Additional mechanisms include leukotriene antagonism and phosphodiesterase inhibition. Its effects may take 6–12 weeks to become apparent[1][5][6].

Brand names
ZaditorAlawayClaritin EyeZyrtec Itchy EyeRefresh Eye Itch Relief
Other names
ketotifen fumarate
02

Targets

CysLTR (Cysteinyl leukotriene receptor family)PDE (Phosphodiesterase family)HRH1 (Histamine H1 Receptor)

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