Preclinical Pharmacology of Bilastine,??a New Selective Histamine??H1 ??Receptor Antagonist

Abstract

These preclinical studies provide evidence that bilastine has H1- antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.

Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans

“…The efficacy of bilastine is supported by preclinical studies in vitro and in experimental animals in vivo showing bilastine to be a potent H 1 -antihistamine [12,13]. It is also supported by a study of 525 patients with chronic idiopathic urticaria in which 20 mg of bilastine once daily was of similar efficacy to 5 mg levocetirizine [14].…”

“…In vitro studies [12] have shown bilastine to have moderate to high affinity and potent activity at the histamine H 1 -receptor while having negligible affinity or effects at 30 different receptors including serotonin, bradykinin, LTD 4 , calcium, muscarinic, a 1 , b 2 , H 2 , H 3 and H 4 receptors. These results are supported by in-vivo studies in experimental animals [13] which also showed bilastine to be rapidly absorbed following oral dosing and to have a long duration of action.…”

The effects of bilastine compared with cetirizine, fexofenadine, and placebo on allergen-induced nasal and ocular symptoms in patients exposed to aeroallergen in the Vienna Challenge Chamber

“…Both cetirizine and fexofenadine are well established in the treatment of allergic rhinitis [7,8] while bilastine is a newly developed drug. Preclinical studies have shown that bilastine is a potent H 1 -antihistamine with a high selectivity for H 1 -receptors and poor or no affinity for other receptors, including serotonin, bradykinin, leukotriene-D 4 , muscarinic M 3 -receptors, a 1 -adrenoceptors, b 2 -adrenoceptors, and H 2 -and H 3 -histamine receptors [9]. By use of the Shultz-Dale reaction, bilastine has also been shown to have anti-inflammatory properties [9].…”

“…Preclinical studies have shown that bilastine is a potent H 1 -antihistamine with a high selectivity for H 1 -receptors and poor or no affinity for other receptors, including serotonin, bradykinin, leukotriene-D 4 , muscarinic M 3 -receptors, a 1 -adrenoceptors, b 2 -adrenoceptors, and H 2 -and H 3 -histamine receptors [9]. By use of the Shultz-Dale reaction, bilastine has also been shown to have anti-inflammatory properties [9]. In clinical studies, bilastine has been shown to have a rapid onset of action and a long duration of effect [10,11].…”

The role and choice criteria of antihistamines in allergy management – Expert opinion

“…None of the conducted clinical trials showed any influence of bilastine on the morphology of the ECG signal and QTc interval. Thus, it could be stated that the cardiovascular safety of bilastine is very high, and the influence of the drug on morphology of the ECG signal and cardiac muscle repolarization is the same as that of placebo [10,15,[32][33][34][35][36][37][38][39][40][41][42][43][44].…”