Bilastine

• CAT Number: I002553
• CAS Number: 202189-78-4
• Molecular Formula: C28H37N3O3
• Molecular Weight: 463.61
• Purity: ≥95%
• Synonyms: 2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
• Target: Histamine Receptor
• Solubility: DMSO: ≥ 49.3 mg/mL
• Storage: Store at -20°C
• IUPAC Name: 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
• InChI: InChI=1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33)
• InChIKey: ACCMWZWAEFYUGZ-UHFFFAOYSA-N
• SMILES: CCOCCN1C2=CC=CC=C2N=C1C3CCN(CC3)CCC4=CC=C(C=C4)C(C)(C)C(=O)O

Bilastine (CAT: I002553) is a second-generation antihistamine that is commonly used for the treatment of allergic rhinitis and chronic urticaria (hives). It acts by selectively blocking histamine H1 receptors, thereby reducing the effects of histamine, a substance involved in allergic reactions. Bilastine provides relief from symptoms such as sneezing, itching, runny nose, and nasal congestion associated with allergic rhinitis. It also helps alleviate the itching and redness associated with chronic urticaria. Bilastine has a favorable profile with minimal sedative effects compared to older-generation antihistamines, making it suitable for daily use without significant impairment of daily activities.

Overview of Clinical Research

Bilastine is a histamine H1 receptor antagonist. Faes Farma completed a phase III trial in Allergic conjunctivitis in Hungary, Lithuania, Poland and Slovakia(Ophthalmic) (EudraCT2018-002248-95) in 2020.

Reference

1: Sádaba Díaz de Rada B, Azanza Perea JR, Gomez-Guiu Hormigos A. Bilastine for the relief of allergy symptoms. Drugs Today (Barc). 2011 Apr;47(4):251-62. doi: 10.1358/dot.2011.47.4.1587029. Review. PubMed PMID: 21573249.
2: Dávila I, Sastre J, Mullol J, Montoro J, Jáuregui I, Ferrer M, del Cuvillo A, Bartra J, Valero A. Effect of bilastine upon nasal obstruction. J Investig Allergol Clin Immunol. 2011;21 Suppl 3:2-8. Review. PubMed PMID: 22185044.
3: Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A. In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist. Drugs R D. 2006;7(4):219-31. PubMed PMID: 16784247.
4: Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A. Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D. 2005;6(6):371-84. PubMed PMID: 16274260.