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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
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

Bilastine

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.


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DMF Number : 39332

Submission : 2023-12-29

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Lee Pharma Ltd

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DMF Number : 36288

Submission : 2021-09-16

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Bilastine (1H)

Date of Issue : 2022-07-28

Valid Till : 2025-06-16

Written Confirmation Number : WC-0036

Address of the Firm : Sy. No. 347,473,474, 490/2 Bonthapally village, Veerabhadraswamy Temple Road, Ji...

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Lee Pharma

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Bilastine IH

Date of Issue : 2020-05-29

Valid Till : 2022-07-28

Written Confirmation Number : WC-0186A4

Address of the Firm : Sy. No. 10/G-1, Gaddapotharam Village, Jinnaram Mandal, Medak Dist, AP

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Bilastine IH

Date of Issue : 2019-10-15

Valid Till : 2022-08-08

Written Confirmation Number : WC-0383A4

Address of the Firm : Sy. No.455/A, 455/AA, 455/E & 455/EE Chandampet Village Shankarampet Mandal Meda...

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Bilastine IH

Date of Issue : 2022-06-23

Valid Till : 2025-04-12

Written Confirmation Number : WC-0525A1

Address of the Firm : Sy. No. 888 & 901, Jangampelle Village,\r\nBhiknoor Mandai, Kamareddy Dist, Tela...

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Bilastine IH

Date of Issue : 2022-06-24

Valid Till : 2025-07-14

Written Confirmation Number : WC-0130n

Address of the Firm : Plot No. 79B, 80A, 80B, 81A, & 82, Kolhar Industrial Area , Bidar, Karnataka -58...

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Bilastine IH

Date of Issue : 2019-07-22

Valid Till : 2022-07-14

Written Confirmation Number : WC-0130A

Address of the Firm : 80-B &81-A, Kolhar Industrial Area, Bidar, Karnataka-585 403

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Symed Labs

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Bilastine IH

Date of Issue : 2021-06-22

Valid Till : 2022-08-08

Written Confirmation Number : WC-0382A4

Address of the Firm : Unit -I Sy. No. 353 Domaguda Village Jinnaram Mandal Medak Dist T.S India

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API Reference Price

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04-Jan-2021
30-Aug-2024
KGS
overview
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Average Price (USD/KGS)

Number of Transactions

Total Quantity (KGS)

Total Value (USD)

Quantity (KGS) & Unit rate (USD/KGS) over time

API Imports and Exports

Importing Country Total Quantity
(KGS)
Average Price
(USD/KGS)
Number of Transactions

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