Chemical Property of Bilastine
Chemical Property:
- Vapor Pressure:3.29E-17mmHg at 25°C
- Melting Point:202 °C
- Boiling Point:639.1°Cat760mmHg
- PKA:4.40±0.10(Predicted)
- Flash Point:340.3°C
- PSA：67.59000
- Density:1.16g/cm3
- LogP:4.79500
- Storage Temp.:Sealed in dry,Room Temperature
- Water Solubility.:Insoluble in water
- XLogP3:2.3
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:10
- Exact Mass:463.28349205
- Heavy Atom Count:34
- Complexity:641
- Purity/Quality:
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99%, *data from raw suppliers
Bilastine
>98.0%(HPLC)(T) *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CCOCCN1C2=CC=CC=C2N=C1C3CCN(CC3)CCC4=CC=C(C=C4)C(C)(C)C(=O)O
- Recent ClinicalTrials:Study to Assess the Safety, Tolerability and Efficacy of Bilastine Ophthalmic Solution 0.6% in Children
- Recent EU Clinical Trials:A multicentre, open-label clinical trial to assess plasma levels and safety of bilastine in children from 2 to 5 years of age with seasonal and/or perennial allergic rhinoconjunctivitis or urticaria
- Recent NIPH Clinical Trials:Efficacy of bilastine on switching treatment in patients with chronic spontaneous urticaria: A comparison study
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Description
Bilastine, a potent and selective histamine H1 receptor antagonist, was
approved in Europe in 2010 for the treatment of allergic rhinoconjunctivitis
(AR) and urticaria (hives or skin rash). The original synthesis of bilastine involves alkylation of 2-piperidinyl-1H-benzimidazole with a phenethyltosylate,
the para position of which is substituted with a dimethyloxazoline
moiety serving as a masked carboxylic acid group. Alkylation of the
benzimidazole nitrogen with 2-chloroethyl ethyl ether followed by
unmasking of the oxazoline moiety with sulfuric acid provided bilastine.In two major clinical trials, bilastine was effective
at relieving allergic rhinitis as assessed by measuring the severity of nasal (obstruction, rhinorrhea, itching, sneezing) and nonnasal (ocular
itching, tearing, ocular redness, itching of ears, and/or palate) symptoms. Bilastine is a histamine H1 receptor antagonist (IC50 = 180 nM). 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. 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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Uses
Bilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria. Labelled Bilastine. It is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
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Clinical Use
Bilastine is a selective histamine H1 antagonist approved for the
treatment of allergic rhinoconjunctivitis and urticaria (hives). This drug, which has proven to be well tolerated in toxicology profiling,
46 was discovered by the Spainsh firm FAES Farma and was
approved by the European Union in 2010.
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Drug interactions
Potentially hazardous interactions with other drugs
Antivirals: concentration possibly increased by
ritonavir.
Grapefruit juice: concentration of bilastine reduced.
