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Details

Stereochemistry ACHIRAL
Molecular Formula C28H37N3O3
Molecular Weight 463.6127
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BILASTINE

SMILES

CCOCCn1c2ccccc2nc1C3CCN(CCc4ccc(cc4)C(C)(C)C(=O)O)CC3

InChI

InChIKey=ACCMWZWAEFYUGZ-UHFFFAOYSA-N
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)

HIDE SMILES / InChI

Molecular Formula C28H37N3O3
Molecular Weight 463.6127
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/25878559 | https://medical.azureedge.net/pdf/28433.pdf?v=636220857643656872 | https://www.faesfarma.com/wp-content/uploads/2015/07/AI-20110329-EN.pdf

Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine is an H1 receptor inverse agonist. Bilastine also exerts anti-inflammatory activity by inhibiting the release of histamine, IL-4 and tumor necrosis factor (TNF)-α from human mast cells and granulocytes. Common side effects are headache and drowsiness.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
64.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Bilaxten

Approved Use

Bilastine is used to relieve the symptoms of hayfever (sneezing, itchy, runny, blocked-up nose and red and watery eyes) and other forms of allergic rhinitis. It may also be used to treat itchy skin rashes (hives or urticaria).

Launch Date

1.2838176E12
Palliative
Bilaxten

Approved Use

Bilastine is used to relieve the symptoms of hayfever (sneezing, itchy, runny, blocked-up nose and red and watery eyes) and other forms of allergic rhinitis. It may also be used to treat itchy skin rashes (hives or urticaria).

Launch Date

1.2838176E12
Palliative
Bilaxten

Approved Use

Bilastine is used to relieve the symptoms of hayfever (sneezing, itchy, runny, blocked-up nose and red and watery eyes) and other forms of allergic rhinitis. It may also be used to treat itchy skin rashes (hives or urticaria).

Launch Date

1.2838176E12
PubMed

PubMed

TitleDatePubMed
Comparative efficacy of bilastine, levocetirizine and desloratadine updosing in chronic urticaria.
2016
Bilastine in allergic rhinoconjunctivitis and urticaria: a practical approach to treatment decisions based on queries received by the medical information department.
2017
Corrigendum to "Application of Analytical Quality by Design concept for bilastine and its degradation impurities determination by hydrophilic interaction liquid chromatographic method" [J. Pharm. Biomed. Anal. 125 (2016) 385-393].
2017 May 10
Patents

Sample Use Guides

20 mg daily
Route of Administration: Oral
Bilastine gave mild positive results for two uptake transporters, OATP2B1 and OCT1, mainly located in liver and intestine. Bilastine IC50 was determined for these two transporters and (based in previous knowledge), also for P-gp. The assay was carried out at seven bilastine concentrations ranging from 0.41 to 300 M. Bilastine showed poor inhibition, as values of IC50 obtained for all the three transporters were ≥ 300 M.
Substance Class Chemical
Created
by admin
on Sat Jun 26 16:38:59 UTC 2021
Edited
by admin
on Sat Jun 26 16:38:59 UTC 2021
Record UNII
PA1123N395
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BILASTINE
INN   MI   WHO-DD  
INN  
Official Name English
BILASTINE [JAN]
Common Name English
BILASTINE [MI]
Common Name English
P-(2-(4-(1-(2-ETHOXYETHYL)-2-BENZIMIDAZOLYL)PIPERIDINO)ETHYL)-.ALPHA.-METHYLHYDRATROPIC ACID
Common Name English
BILASTINE [INN]
Common Name English
BILASTINE [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29578
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
WHO-VATC QR06AX29
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
WHO-ATC R06AX29
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
Code System Code Type Description
DRUG BANK
DB11591
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
NCI_THESAURUS
C73045
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
PUBCHEM
185460
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
MESH
C445659
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
CAS
202189-78-4
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
DRUG CENTRAL
4353
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
EPA CompTox
202189-78-4
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
ChEMBL
CHEMBL1742423
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
INN
7905
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
EVMPD
SUB37845
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
FDA UNII
PA1123N395
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
MERCK INDEX
M2490
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY Merck Index
WIKIPEDIA
BILASTINE
Created by admin on Sat Jun 26 16:39:00 UTC 2021 , Edited by admin on Sat Jun 26 16:39:00 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY