Bilastine

Bilastine
Clinical data
Trade names	Blexten, others
Pregnancy; category	AU: B3;
Routes of; administration	By mouth
Drug class	Antihistamine
ATC code	R06AX29 (WHO) S01GX13 (WHO);
Legal status
Legal status	AU: S2 (Pharmacy medicine); CA: ℞-only; NZ: S2 (Pharmacy Only);
Pharmacokinetic data
Bioavailability	61%
Protein binding	84-90% binding to plasma proteins
Metabolism	Not significantly metabolised
Onset of action	1 hour (Allertine)
Elimination half-life	14.5 hours
Duration of action	24 hours (Allertine)
Excretion	95% in urine and faeces
Identifiers
	IUPAC name 2-[4-(2-{4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid;
CAS Number	202189-78-4 ;
PubChem CID	185460;
DrugBank	DB11591;
ChemSpider	161234 ;
UNII	PA1123N395;
KEGG	D09570;
ChEMBL	ChEMBL1742423 ;
CompTox Dashboard (EPA)	DTXSID5057678 ;
ECHA InfoCard	100.260.016
Chemical and physical data
Formula	C28H37N3O3
Molar mass	463.622 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(O)C(c1ccc(cc1)CCN4CCC(c2nc3ccccc3n2CCOCC)CC4)(C)C;
	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) ; Key:ACCMWZWAEFYUGZ-UHFFFAOYSA-N ;
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Bilastine is an antihistamine medication used to treat hives (urticaria), allergic rhinitis and itchy inflamed eyes (allergic conjunctivitis) caused by an allergy. It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H₁ receptor, preventing these allergic reactions. Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.

Bilastine was discovered by the Spanish firm FAES Farma and received its first approval in the European Union in 2010 for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. It is also approved in Canada and Australia. As of 2023, it remained unapproved for any use in the United States, although Hikma Pharmaceuticals had agreed in 2021 to begin the FDA approval process.

Evidence has shown that bilastine is effective in treating skin and eye symptoms of allergic reactions, improving patient's quality of life. Bilastine meets the treatment criteria for allergic rhinitis, as published by the European Academy of Allergy and Clinical Immunology (EAACI) and the Allergic Rhinitis and its Impact on Asthma (ARIA) initiative.

Clinical data

Trade names	Blexten, others
Pregnancy category	AU: B3
Routes of administration	By mouth
Drug class	Antihistamine
ATC code	R06AX29 (WHO) S01GX13 (WHO)
Legal status
Legal status	AU: S2 (Pharmacy medicine) CA: ℞-only NZ: S2 (Pharmacy Only)
Pharmacokinetic data
Bioavailability	61%
Protein binding	84-90% binding to plasma proteins
Metabolism	Not significantly metabolised
Onset of action	1 hour (Allertine)
Elimination half-life	14.5 hours
Duration of action	24 hours (Allertine)
Excretion	95% in urine and faeces
Identifiers
IUPAC name 2-[4-(2-{4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid
CAS Number	202189-78-4^Y
PubChem CID	185460
DrugBank	DB11591
ChemSpider	161234^Y
UNII	PA1123N395
KEGG	D09570
ChEMBL	ChEMBL1742423^Y
CompTox Dashboard (EPA)	DTXSID5057678
ECHA InfoCard	100.260.016
Chemical and physical data
Formula	C₂₈H₃₇N₃O₃
Molar mass	463.622 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES O=C(O)C(c1ccc(cc1)CCN4CCC(c2nc3ccccc3n2CCOCC)CC4)(C)C
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)^Y Key:ACCMWZWAEFYUGZ-UHFFFAOYSA-N^Y
^NY (what is this?) (verify)