1. 202189-78-4
2. Ilaxten
3. 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic Acid
4. Bilastina
5. Dtxsid5057678
6. Pa1123n395
7. Dtxcid6031467
8. Bilastinum
9. P-(2-(4-(1-(2-ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-alpha-methylhydratropic Acid
10. 2-[4-(2-{4-[1-(2-ethoxyethyl)-1h-1,3-benzodiazol-2-yl]piperidin-1-yl}ethyl)phenyl]-2-methylpropanoic Acid
11. 2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-1,3-benzodiazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic Acid
12. 2-(4-(2-(4-(1-(2-ethoxyethyl)benzimidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic Acid
13. Refchem:568338
14. R06ax29
15. Bilaxten
16. Bilastine [inn]
17. 2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic Acid
18. Mfcd09837814
19. Benzeneacetic Acid, 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethyl-
20. C28h37n3o3
21. Bilasten
22. Bilatex
23. Bilastine?
24. Unii-pa1123n395
25. 2-[4-[2-[4-[1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic Acid
26. Bilanoa (tn)
27. Bilastine (standard)
28. F-96221-bm1
29. Bilastine (jan/inn)
30. Bilastine [jan]
31. Bilastine [mi]
32. Bilastine [who-dd]
33. Schembl991810
34. Orb1303023
35. Chembl1742423
36. Schembl29402994
37. Gtpl11579
38. Accmwzwaefyugz-uhfffaoysa-n
39. Chebi:135954
40. Glxc-07503
41. Hms3887o17
42. Hms5087e16
43. Ex-a2962
44. Msk14409
45. Tox21_113905
46. Hy-14447r
47. S3721
48. Akos030241723
49. Ccg-269384
50. Db11591
51. F-96221-bm
52. Sb17508
53. Ncgc00262907-01
54. 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]-1-piperidyl]ethyl]phenyl]-2-methyl-propanoic Acid
55. Ac-29231
56. Bs-15792
57. Da-51119
58. Hy-14447
59. Sy234324
60. B5392
61. Cas-202189-78-4
62. Ns00040658
63. D09570
64. 189b784
65. En300-19634515
66. F803285
67. Q2902977
68. Brd-k51937257-001-01-4
69. 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1h-benzoimidazol-2-yl]-piperidin-1-yl}-ethyl)-phenyl]-2-methyl-propionic Acid
70. 2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1h-benzoimidazol-2-yl]-piperidin-1-yl}ethyl)-phenyl]-2-methyl-propionic Acid
71. 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethylbenzeneacetic Acid; Bilastine
72. Benzeneacetic Acid, 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-
73. A,
74. A-dimethyl-
75. P-(2-(4-(1-(2-ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-.alpha.-methylhydratropic Acid
| Molecular Weight | 463.6 g/mol |
|---|---|
| Molecular Formula | C28H37N3O3 |
| XLogP3 | 2.3 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 10 |
| Exact Mass | Da |
| Monoisotopic Mass | Da |
| Topological Polar Surface Area | 67.6 |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 641 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
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 conjunctivitis
Treatment of acute type I hypersensitivity reactions
Treatment of allergic rhinoconjunctivitis, Treatment of urticaria
Treatment of urticaria, Treatment of allergic rhinoconjunctivitis
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. (2021) DOI:10.1021/acsenvironau.1c00008. 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
ATCvet Code
QR - Respiratory system
QR06 - Antihistamines for systemic use
QR06A - Antihistamines for systemic use
QR06AX - Other antihistamines for systemic use
QR06AX29 - Bilastine
ATCvet Code
QS - Sensory organs
QS01 - Ophthalmologicals
QS01G - Decongestants and antiallergics
QS01GX - Other antiallergics
QS01GX13 - Bilastine
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.
Bilastine does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans.
The mean half life of elimination is 14.5h.
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.
