Bilastine - CAS 202189-78-4
Catalog number: 202189-78-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Histamine Receptor
Bilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
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Bilastine, trade name Bilaxten
1. Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans
Martin K. Church. Inflamm. Res. (2011) 60:1107–1112
Early clinical trials have also shown bilastine to be a potent and effective H1-antihistamine. In a study of 525 patients with chronic idiopathic urticaria, bilastine 20 mg once daily significantly (P<0.001 compared with pla- cebo) relieved the symptoms. Furthermore, the overall efficacy results demonstrated that bilastine was of similar efficacy to levocetirizine. In the nose, a double-blind cross-over study in which 75 allergic volunteers were challenged with grass pollen in the Vienna Challenge Chamber showed bilastine to be equally effective as cetirizine and fexofenadine but the results obtained suggest that it has a longer duration than fexofenadine, while in two 14-day trials in seasonal allergic rhinitis, bilastine was shown to be of similar efficacy to daily dosage with 10 mg cetirizine and 5 mg desloratadine.
2. Allergic Conjunctivitis and the Impact of Allergic Rhinitis
Leonard Bielory. Curr Allergy Asthma Rep (2010) 10:122–134
Antihistamines: Bilastine and Bepotastine Recent clinical data suggest an ocular and nasal allergy efficacy profile for bilastine, a new oral antihistamine, similar to that of established oral antihistamines, including desloratadine and cetirizine. In addition, another oral antihistamine agent, bepotastine, was shown to be effective and well-tolerated in patients with Japanese cedar allergen–induced symptoms in an exposure chamber and was recently approved in the United States in an ophthalmic formulation with a very similar profile to those of olopatadine and epinastine.
3. New Therapies for Allergic Rhinitis
Fulvio Braido & Francesca Sclifò & Matteo Ferrando & Giorgio Walter Canonica. Curr Allergy Asthma Rep (2014) 14:422
Bilastine, a new nonsedating H1 receptor inverse agonist, belongs to the piperidine class along with loratadine, desloratadine, and fexofenadine. In vitro studies have shown that bilastine has a high specific affinity for the H1 receptor but no or very low affinity for 30 other tested receptors. This affinity for the H1 receptor is three and six times higher than for cetirizine and fexofenadine, respectively. Bilastine behaves as an H1 mixed antagonist (competitive up to 33 nM; not competitive from 100 nM), as it is 5.5 times more powerful than cetirizine as a competitive antagonist and 10 times more powerful as a noncompetitive antagonist. The effectiveness of bilastine is comparable to that of desloratadine. Besides its H1 antagonism, bilastine has also demonstrated anti-inflammatory properties, including inhibiting the release of proinflammatory cytokines such as IL-4 and tumor necrosis factor-α. Furthermore, in vivo studies in rats demonstrated a significant reduction in histamine-stimulated endothelial permeability, microvascular extravasation, and inhibition of smooth muscular contraction and bronchospasm times that of cetirizine.
4. Integration of preclinical and clinical knowledge to predict intravenous PK in human: Bilastine case study
Valvanera Vozmediano • Ignacio Ortega • John C. Lukas • Ana Gonzalo • Monica Rodriguez • Maria Luisa Lucero. Eur J Drug Metab Pharmacokinet (2014) 39:33–41
First PK modeling was performed for the i.v. and p.o. data in animals alone. Two compartmental representations best described the kinetics of bilastine in animals. The results of Jauregizar et al. (2009) were applied for p.o. bilastine in man. The PK parameters for all species are listed in Table 3 (for p.o. in rat, dog and man and for i.v. in rat and dog). Table 3 also lists the protein binding fraction (fu) for bilastine in these three species.
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CAS 202189-78-4 Bilastine

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