Bilastine
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MedKoo CAT#: 314243

CAS#: 202189-78-4

Description: Bilastine (trade name Bilaxten) is a second generation antihistamine drug for the treatment of allergic rhinoconjunctivitis and urticaria (hives). It exerts its effect as a selective histamine H1 receptor antagonist, and has a potency similar to cetirizine and is superior to fexofenadine. It was developed in Spain by FAES Farma. Bilastine is approved in the European Union for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria, but it is not approved by the U.S. Food and Drug Administration for any use in the United States. Bilastine has been effective in the treatment of ocular symptoms and diseases of allergies, including rhinoconjuctivitis. Additionally, bilastine has been shown to improve quality of life, and all nasal and ocular symptoms related to allergic rhinitis.


Price and Availability

Size Price Shipping out time Quantity
200mg USD 150 Same day
500mg USD 350 Same day
1g USD 630 Same day
2g USD 1130 Same day
5g USD 2450 Same day
10g USD 4350 Same day
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

Bilastine, purity > 98%, is in stock. The same day shipping after order received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 314243
Name: Bilastine
CAS#: 202189-78-4
Chemical Formula: C28H37N3O3
Exact Mass: 463.28349
Molecular Weight: 463.61
Elemental Analysis: C, 72.54; H, 8.04; N, 9.06; O, 10.35


Synonym: Bilastine trade name Bilaxten

IUPAC/Chemical Name: 2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid

InChi Key: ACCMWZWAEFYUGZ-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: CC(C)(C1=CC=C(CCN2CCC(C3=NC4=CC=CC=C4N3CCOCC)CC2)C=C1)C(O)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO.

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2933998090


References

1: Farré M, Pérez-Mañá C, Papaseit E, Menoyo E, Pérez M, Martin S, Bullich S, Rojas S, Herance JR, Trampal C, Labeaga L, Valiente R. Bilastine vs. Hydroxyzine: Occupation of Brain Histamine H(1) Receptors Evaluated by Positron Emission Tomography in Healthy Volunteers. Br J Clin Pharmacol. 2014 May 15. doi: 10.1111/bcp.12421. [Epub ahead of print] PubMed PMID: 24833043.

2: García-Gea C, Martínez J, Ballester MR, Gich I, Valiente R, Antonijoan RM. Psychomotor and subjective effects of bilastine, hydroxyzine, and cetirizine, in combination with alcohol: a randomized, double-blind, crossover, and positive-controlled and placebo-controlled Phase I clinical trials. Hum Psychopharmacol. 2014 Mar;29(2):120-32. doi: 10.1002/hup.2378. Epub 2014 Jan 3. PubMed PMID: 24395298.

3: Wolthers OD. Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria. Biomed Res Int. 2013;2013:626837. doi: 10.1155/2013/626837. Epub 2013 Jul 14. PubMed PMID: 23956994; PubMed Central PMCID: PMC3728546.

4: Lasseter KC, Sologuren A, La Noce A, Dilzer SC. Evaluation of the single-dose pharmacokinetics of bilastine in subjects with various degrees of renal insufficiency. Clin Drug Investig. 2013 Sep;33(9):665-73. doi: 10.1007/s40261-013-0110-0. PubMed PMID: 23873362; PubMed Central PMCID: PMC3751212.

5: Krause K, Spohr A, Zuberbier T, Church MK, Maurer M. Up-dosing with bilastine results in improved effectiveness in cold contact urticaria. Allergy. 2013 Jul;68(7):921-8. doi: 10.1111/all.12171. Epub 2013 Jun 6. PubMed PMID: 23742030; PubMed Central PMCID: PMC3759706.

6: Jáuregui I, Ferrer M, Bartra J, del Cuvillo A, Dávila I, Montoro J, Mullol J, Sastre J, Valero A. Bilastine for the treatment of urticaria. Expert Opin Pharmacother. 2013 Aug;14(11):1537-44. doi: 10.1517/14656566.2013.800044. Epub 2013 May 16. Review. PubMed PMID: 23675825.

7: Sadaba B, Azanza JR, Gomez-Guiu A, Rodil R. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria. Ther Clin Risk Manag. 2013;9:197-205. doi: 10.2147/TCRM.S16079. Epub 2013 May 3. PubMed PMID: 23667312; PubMed Central PMCID: PMC3650569.

8: Vozmediano V, Ortega I, Lukas JC, Gonzalo A, Rodriguez M, Lucero ML. Integration of preclinical and clinical knowledge to predict intravenous PK in human: bilastine case study. Eur J Drug Metab Pharmacokinet. 2014 Mar;39(1):33-41. doi: 10.1007/s13318-013-0131-3. Epub 2013 Apr 26. PubMed PMID: 23619917.

9: Sádaba B, Gómez-Guiu A, Azanza JR, Ortega I, Valiente R. Oral availability of bilastine. Clin Drug Investig. 2013 May;33(5):375-81. doi: 10.1007/s40261-013-0076-y. PubMed PMID: 23529786.

10: Duh D, Tanret I. [Bilastine [Bellozal), oral]. J Pharm Belg. 2012 Dec;(4):53-4. French. PubMed PMID: 23350212.