Bilastine

Bilastine
Clinical data
Trade namesBlexten, others
Pregnancy
category
Routes of
administration		By mouth
Drug classAntihistamine
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability61%[1]
Protein binding84-90% binding to plasma proteins[1]
MetabolismNot significantly metabolised[1]
Onset of action1 hour (Allertine)[1]
Elimination half-life14.5 hours[1]
Duration of action24 hours (Allertine)[1]
Excretion95% in urine and faeces[1]
Identifiers
  • 2-[4-(2-{4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.260.016 Edit this at Wikidata
Chemical and physical data
FormulaC28H37N3O3
Molar mass463.622 g·mol−1
3D model (JSmol)
  • O=C(O)C(c1ccc(cc1)CCN4CCC(c2nc3ccccc3n2CCOCC)CC4)(C)C
  • 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) checkY
  • Key:ACCMWZWAEFYUGZ-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Bilastine is an antihistamine medication used to treat hives (urticaria), allergic rhinitis and itchy inflamed eyes (allergic conjunctivitis) caused by an allergy.[6] It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions.[7] Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.[8]

Bilastine is approved in the European Union, Canada and Australia for the symptomatic treatment of allergic conjunctivitis and urticaria.[9] As of 2023, it remained unapproved for any use in the United States,[10] although Hikma Pharmaceuticals had agreed in 2021 to begin the FDA approval process.[11]

Evidence has shown that bilastine is effective in treating skin and eye symptoms of allergic reactions, improving patient's quality of life.[8][12] 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.[12]

  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.
  5. ^ "bilastine classification". (mcc). Retrieved 17 August 2024.
  6. ^ "Ilaxten 20 mg tablets - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 24 June 2021. Retrieved 16 June 2021.
  7. ^ 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.
  8. ^ a b Cite error: The named reference Bartra was invoked but never defined (see the help page).
  9. ^ 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.
  10. ^ Bilastine Approval Status Archived 2023-08-27 at the Wayback Machine, drugs.com
  11. ^ "Hikma and FAES Farma enter into exclusive licensing agreement for the commercialisation of Bilastine tablets in the US" (Press release). Hikma Pharmaceuticals. 20 Sep 2021. Retrieved 25 Aug 2024.
  12. ^ 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.