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    Bilastine

    ACTIVE PHARMA INGREDIENTS

    DEVELOPMENTS

    INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    DIGITAL CONTENT

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    2D Structure
    Also known as: 202189-78-4, Bilaxten, Ilaxten, Bilastine [inn], 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid, 2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
    Molecular Formula
    C28H37N3O3
    Molecular Weight
    463.6  g/mol
    InChI Key
    ACCMWZWAEFYUGZ-UHFFFAOYSA-N
    FDA UNII
    PA1123N395
    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.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
    2.1.2 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)
    2.1.3 InChI Key
    ACCMWZWAEFYUGZ-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CCOCCN1C2=CC=CC=C2N=C1C3CCN(CC3)CCC4=CC=C(C=C4)C(C)(C)C(=O)O
    2.2 Other Identifiers
    2.2.1 UNII
    PA1123N395
    2.3 Synonyms
    2.3.1 Depositor-Supplied Synonyms

    1. 202189-78-4

    2. Bilaxten

    3. Ilaxten

    4. Bilastine [inn]

    5. 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic Acid

    6. 2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic Acid

    7. Pa1123n395

    8. Bilastinum

    9. Bilatex

    10. Unii-pa1123n395

    11. 2-[4-[2-[4-[1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic Acid

    12. Bilanoa (tn)

    13. Bilastine (jan/inn)

    14. Bilastine [jan]

    15. Bilastine [mi]

    16. Bilastine [who-dd]

    17. Dsstox_cid_31467

    18. Dsstox_rid_97352

    19. Dsstox_gsid_57678

    20. Benzeneacetic Acid,4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-a,a-dimethyl-

    21. Schembl991810

    22. Chembl1742423

    23. Dtxsid5057678

    24. Gtpl11579

    25. Chebi:135954

    26. Hms3887o17

    27. Amy16470

    28. Bcp02576

    29. Ex-a2962

    30. Zinc3822702

    31. Tox21_113905

    32. Mfcd09837814

    33. S3721

    34. Akos030241723

    35. Bcp9000412

    36. Ccg-269384

    37. Db11591

    38. F-96221-bm

    39. Sb17508

    40. Ncgc00262907-01

    41. Ac-29231

    42. Bs-15792

    43. Hy-14447

    44. B5392

    45. Cas-202189-78-4

    46. Ft-0700542

    47. D09570

    48. 189b784

    49. A856214

    50. Q2902977

    51. P-(2-(4-(1-(2-ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-alpha-methylhydratropic Acid

    52. 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1h-benzoimidazol-2-yl]-piperidin-1-yl}-ethyl)-phenyl]-2-methyl-propionic Acid

    53. 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1h-benzoimidazol-2-yl]-piperidin-1-yl}ethyl)-phenyl]-2-methyl-propionic Acid

    54. 2-[4-[2-[4-[1-(2-ethoxyethyl)-1h-benzoimidazole-2-yl]piperidine-1-yl]ethyl]phenyl]-2-methylpropanoic Acid

    55. 2-[4-[2-[4-[1-(2-ethoxyethyl)benzoimidazol-2-yl]-1-piperidyl]ethyl]phenyl]-2-methyl-propanoic Acid

    56. Benzeneacetic Acid, 4-(2-(4-(1-(2-ethoxyethyl)-1h-benzimidazol-2-yl)-1-piperidinyl)ethyl-alpha, Alpha-dimethyl-

    57. Benzeneacetic Acid, 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethyl-

    58. Benzeneaceticacid,4-(2-(4-(1-(2-ethoxyethyl)-1h-benzimidazol-2-yl)-1-piperidinyl)ethyl-alpha,alpha-dimethyl-

    59. Bilastine; 2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic Acid

    60. P-(2-(4-(1-(2-ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-.alpha.-methylhydratropic Acid

    2.4 Create Date
    2005-08-09
    3 Chemical and Physical Properties
    Molecular Weight 463.6 g/mol
    Molecular Formula C28H37N3O3
    XLogP32.3
    Hydrogen Bond Donor Count1
    Hydrogen Bond Acceptor Count5
    Rotatable Bond Count10
    Exact Mass463.28349205 g/mol
    Monoisotopic Mass463.28349205 g/mol
    Topological Polar Surface Area67.6 Ų
    Heavy Atom Count34
    Formal Charge0
    Complexity641
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 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

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

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

    5.2 ATC Code

    R06AX29

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    R - Respiratory system

    R06 - Antihistamines for systemic use

    R06A - Antihistamines for systemic use

    R06AX - Other antihistamines for systemic use

    R06AX29 - Bilastine

    S - Sensory organs

    S01 - Ophthalmologicals

    S01G - Decongestants and antiallergics

    S01GX - Other antiallergics

    S01GX13 - Bilastine

    5.3 Absorption, Distribution and Excretion

    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%.

    Route of Elimination

    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.

    Clearance

    Bilastine has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h.

    5.4 Metabolism/Metabolites

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

    5.5 Biological Half-Life

    The mean half life of elimination is 14.5h.

    5.6 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.