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Bilastine

Bilastine structure

CAS No:
202189-78-4
Formula:
C28H37N3O3
Chemical Name:
Bilastine
Synonyms:
Benzeneacetic acid,4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl-;4-[2-[4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethylbenzeneacetic acid;Bilastine;2-[-4-(2-[4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl)phenyl]-2-methylpropanoic acid
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for h

Bilastine is a member of benzimidazoles.|Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.

Bilastine Basic Attributes

Molecular Weight：

463.61

Exact Mass：

463.61

UNII：

PA1123N395

DSSTox ID：

DTXSID5057678

ATC Code：

R06AX29|R - Respiratory system

Characteristics

PSA：

67.6

XLogP3：

2.3

Density：

1.2±0.1 g/cm3

Boiling Point：

639.1±55.0°C at 760 mmHg

Flash Point：

340.3±31.5 °C

Refractive Index：

1.594

Vapor Pressure：

3.29E-17mmHg at 25°C

Safety Information

Precautionary statement(s)：

P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P322, P330, P363, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P322, P330, P363, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Toxicity

Toxicity Summary：

The most common adverse effects experienced during clinical trials were abdominal pain, dizziness, headache, and somnolence. Bilastine is associated with Q/T prolongation. The no observed adverse effect level of bilastine is 1200 mg/kg/day in rats and 125 mg/kg/day in dogs.

Protein Binding：

Bilastine is 84-90% bound to human plasma proteins.

Drug Information

Drug Indication：

For symptomatic relief of nasal and non-nasal symptoms of seasonal rhinitis in patients 12 years of age and older and for symptomatic relief in chronic spontaneous urticaria in patients 18 years of age and older.|FDA Label|Treatment of allergic rhinoconjunctivitis, Treatment of urticaria|Treatment of urticaria, Treatment of allergic rhinoconjunctivitis|Treatment of acute type I hypersensitivity reactions|Treatment of allergic conjunctivitis

Pharmacology：

Bilastine is an antiallergenic and acts to reduce allergic symptoms such as nasal congestion and urticaria.

Absorption：

Bilastine has a Tmax of 1.13 h. The absolute bioavailability is 61%. No accumulation observed with daily dosing of 20-100 mg after 14 days. Cmax decreased by 25 % and 33% when taken with a low fat and high fat meal compared to fasted state. Administration with grapefruit juice decreased Cmax by 30%.|Bilastine is mainly excreted in the feces (66.5%) with some excreted in the urine (28.3%). Nearly all is excreted as the parent compound.|Bilastine has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h.

Metabolism/Metabolites：

Bilastine does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans.

Biological Half-Life：

The mean half life of elimination is 14.5h.

Mechanism of Action：

Bilastine is a selective histamine H1 receptor antagonist (Ki = 64nM). During allergic response mast cells undergo degranulation which releases histamine and other subastances. By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells.

MeSH Entry Terms：

bilastine

Bilastine Use and Manufacturing

Uses

Labelled Bilastine. It is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

Use Classification：

Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:463.6
XLogP3:2.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:10
Exact Mass:463.28349205
Monoisotopic Mass:463.28349205
Topological Polar Surface Area:67.6
Heavy Atom Count:34
Complexity:641
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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