Bilastine information

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: S3 (Pharmacist only); CA: ℞-only; UK: POM (Prescription 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.^[5] It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H₁ receptor, preventing these allergic reactions.^[6] Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.^[7]

Bilastine is approved in the European Union for the symptomatic treatment of allergic conjunctivitis and urticaria.^[8] It is not approved for any use in the United States.^[9]

Evidence has shown that bilastine is effective in treating skin and eye symptoms of allergic reactions, improving patient's quality of life.^[7]^[10] 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 of Asthma (ARIA) initiative.^[10]

^ ^a ^b ^c ^d ^e ^f ^g ^h "Australian Product Information - Allertine (Bilastine) tablet". Therapeutic Goods Administration. 27 April 2022. Archived from the original on 13 September 2022. Retrieved 13 September 2022.
^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 21 December 2022. Archived from the original on 3 April 2022. Retrieved 2 January 2023.
^ "Public summary - ALLERTINE bilastine 20 mg tablet blister pack". Therapeutic Goods Administration. 27 April 2022. Archived from the original on 7 December 2022. Retrieved 13 September 2022.
^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
^ ^a ^b "Ilaxten 20 mg tablets - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 24 June 2021. Retrieved 16 June 2021.
^ Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A (2005). "Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity". Drugs in R&D. 6 (6): 371–384. doi:10.2165/00126839-200506060-00005. PMID 16274260. S2CID 23407135.
^ ^a ^b Cite error: The named reference Bartra was invoked but never defined (see the help page).
^ Cumulative Nce introduction index, 1983–2010. Annual Reports in Medicinal Chemistry. Vol. 46. 2011. pp. 531–551. doi:10.1016/B978-0-12-386009-5.00035-7. ISBN 9780123860095.
^ Bilastine Approval Status Archived 2023-08-27 at the Wayback Machine, drugs.com
^ ^a ^b Bousquet J, Ansótegui I, Canonica GW, Zuberbier T, Baena-Cagnani CE, Bachert C, et al. (January 2012). "Establishing the place in therapy of bilastine in the treatment of allergic rhinitis according to ARIA: evidence review". Current Medical Research and Opinion. 28 (1): 131–139. doi:10.1185/03007995.2011.648263. PMID 22149770. S2CID 8429174.

[Allertine_TGA_PI-1] ^ ^a ^b ^c ^d ^e ^f ^g ^h "Australian Product Information - Allertine (Bilastine) tablet". Therapeutic Goods Administration. 27 April 2022. Archived from the original on 13 September 2022. Retrieved 13 September 2022.

[2] "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 21 December 2022. Archived from the original on 3 April 2022. Retrieved 2 January 2023.

[3] "Public summary - ALLERTINE bilastine 20 mg tablet blister pack". Therapeutic Goods Administration. 27 April 2022. Archived from the original on 7 December 2022. Retrieved 13 September 2022.

[4] "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.

[Ilaxten_SmPC-5] "Ilaxten 20 mg tablets - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 24 June 2021. Retrieved 16 June 2021.

[6] Corcóstegui R, Labeaga L, Innerárity A, Berisa A, Orjales A (2005). "Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity". Drugs in R&D. 6 (6): 371–384. doi:10.2165/00126839-200506060-00005. PMID 16274260. S2CID 23407135.

[Bartra-7] Cite error: The named reference Bartra was invoked but never defined (see the help page).

[8] Cumulative Nce introduction index, 1983–2010. Annual Reports in Medicinal Chemistry. Vol. 46. 2011. pp. 531–551. doi:10.1016/B978-0-12-386009-5.00035-7. ISBN 9780123860095.

[9] Bilastine Approval Status Archived 2023-08-27 at the Wayback Machine, drugs.com

[Bousquets-10] Bousquet J, Ansótegui I, Canonica GW, Zuberbier T, Baena-Cagnani CE, Bachert C, et al. (January 2012). "Establishing the place in therapy of bilastine in the treatment of allergic rhinitis according to ARIA: evidence review". Current Medical Research and Opinion. 28 (1): 131–139. doi:10.1185/03007995.2011.648263. PMID 22149770. S2CID 8429174.

Bilastine information

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Clinical data

Trade names	Blexten, others
Pregnancy category	AU: B3^[1]^[2]
Routes of administration	By mouth
Drug class	Antihistamine
ATC code	R06AX29 (WHO) S01GX13 (WHO)
Legal status
Legal status	AU: S3 (Pharmacist only)^[3] CA: ℞-only^[4] UK: POM (Prescription only)^[5]
Pharmacokinetic data
Bioavailability	61%^[1]
Protein binding	84-90% binding to plasma proteins^[1]
Metabolism	Not significantly metabolised^[1]
Onset of action	1 hour (Allertine)^[1]
Elimination half-life	14.5 hours^[1]
Duration of action	24 hours (Allertine)^[1]
Excretion	95% in urine and faeces^[1]
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)