Oral cetirizine is one of the most used oral medications for treatment of allergic rhinitis. In May 2017, the FDA approved the first ophthalmic formulation of the second-generation histamine-1 (H1) receptor antagonist for use in treating ocular itching associated with allergic conjunctivitis.
The approval was based on an NDA package that included data demonstrating the efficacy, safety, and tolerability of cetirizine ophthalmic solution 0.24% (Zerviate, Nicox) in 3 phase III randomized, double-masked, vehicle-controlled clinical trials using the conjunctival antigen challenge (CAC) model.
The results showed that cetirizine had a rapid onset of action for mitigating allergen-induced conjunctival itching and prolonged activity, demonstrating statistically and clinically significant superiority to vehicle at evaluations performed 15 minutes and 8 hours after instillation of the topical drop.
Cetirizine is recommended for twice daily dosing, and its safety and effectiveness were established in pediatric patients 2 years of age and older.
“We are excited to bring this product to market because it is the only topical ocular antihistamine containing cetirizine, an active ingredient with a long track record of safe and effective oral use,” said Michele Garufi, chairman and CEO, Nicox, Valbonne, France. “Cetirizine has been available for oral use for over 20 years. The compound is well known to ophthalmologists, allergists, pediatricians, and other primary care providers.”