Bilastine

Bilastine is a histamine H₁ receptor antagonist (IC₅₀ = 180 nM).¹ It is selective for the histamine H₁ receptor in a panel of 30 receptors in vitro at 100 µM. Bilastine prevents microvascular extravasation (ED₅₀ = 185 µg/kg, i.v.), bronchospasm (ED₅₀ = 4.6 µg/kg, i.v.), and systemic anaphylaxis (ED₅₀ = 0.2 µg/kg, p.o.) induced by subcutaneous histamine in guinea pigs.² It prevents anaphylaxis induced by subcutaneous administration of ovalbumin or dinitrophenylated human albumin (DNP) in sensitized rats when administered at doses of 7.6 and 6.0 mg/kg, respectively. Formulations containing bilastine have been used in the treatment of urticaria and allergic rhinitis.

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1. Corcóstegui, R., Labeaga, L., Innerárity, A., et al. Preclinical pharmacology of bilastine, a new selective histamine H₁ receptor antagonist: Receptor selectivity and in vitro antihistaminic activity. Drugs R. D. 6(6), 371-384 (2005).

2. Corcóstegui, R., Labeaga, L., Innerárity, A., et al. In vivo pharmacological characterisation of bilastine, a potent and selective histamine H₁ receptor antagonist. Drugs R. D. 7(4), 219-231 (2006).