Bepotastine Besilate

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 317317

CAS#: 125602-71-3

Description: Bepotastine besilate is a second generation antihistamine. Bepostatine besilate is used to treat allergic rhinitis and urticaria and pruritus. Bepotastine besilate inhibits the action of histamine by blocking histamine H1 receptors, antagonising the vasoconstrictor, and to a lesser extent, the vasodilator effects of histamine. Mast cell stabilisers inhibit degranulation and consequently the release of histamine by interrupting the normal chain of intracellular signals. The brand of Bepostatine besilate is Talion.

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Bepotastine Besilate, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 317317
Name: Bepotastine Besilate
CAS#: 125602-71-3
Chemical Formula: C27H31ClN2O6S
Exact Mass:
Molecular Weight: 547.06
Elemental Analysis: C, 59.28; H, 5.71; Cl, 6.48; N, 5.12; O, 17.55; S, 5.86

Synonym: Bepotastine Besilate; Bepreve; Talion; Bepotastine besylate

IUPAC/Chemical Name: benzenesulfonic acid;4-[4-[(S)-(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid


InChi Code: InChI=1S/C21H25ClN2O3.C6H6O3S/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26;7-10(8,9)6-4-2-1-3-5-6/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26);1-5H,(H,7,8,9)


Technical Data

Solid powder

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

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).

Soluble in DMSO, not in water

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).

Harmonized System Code:


1: Okubo K, Ichimura M, Koyama T, Susuta Y, Izaki H. Double-blind
placebo-controlled study of bepotastine besilate in pediatric patients with
perennial allergic rhinitis. Expert Opin Pharmacother. 2015 Sep 12:1-14. [Epub
ahead of print] PubMed PMID: 26364765.

2: Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A. Topical
antihistamines and mast cell stabilisers for treating seasonal and perennial
allergic conjunctivitis. Cochrane Database Syst Rev. 2015 Jun 1;6:CD009566. doi:
10.1002/14651858.CD009566.pub2. Review. PubMed PMID: 26028608.

3: Lim DS, Youn YS, Kwack SJ, Kwak HM, Lim SK, Kim JY, Um YM, Lee JD, Hyeon JH,
Kim YJ, Kim HS, Lee BM. Comparative efficacy and bioequivalence of novel
h1-antihistamine bepotastine salts (nicotinate and salicylate). J Toxicol Environ
Health A. 2014;77(22-24):1451-66. doi: 10.1080/15287394.2014.955833. PubMed PMID:

4: Bergmann MT, Williams JI, Gomes PJ. Treatment of allergic conjunctivitis with
bepotastine besilate ophthalmic solution 1.5%. Clin Ophthalmol. 2014 Aug
13;8:1495-505. doi: 10.2147/OPTH.S66637. eCollection 2014. PubMed PMID: 25152611;
PubMed Central PMCID: PMC4140238.

5: Kim MY, Jo EJ, Chang YS, Cho SH, Min KU, Kim SH. A case of
levocetirizine-induced fixed drug eruption and cross-reaction with piperazine
derivatives. Asia Pac Allergy. 2013 Oct;3(4):281-4. doi:
10.5415/apallergy.2013.3.4.281. Epub 2013 Oct 31. PubMed PMID: 24260733; PubMed
Central PMCID: PMC3826602.

6: Bielory L, Duttachoudhury S, McMunn A. Bepotastine besilate for the treatment
of pruritus. Expert Opin Pharmacother. 2013 Dec;14(18):2553-69. doi:
10.1517/14656566.2013.849242. Epub 2013 Nov 5. Review. PubMed PMID: 24191914.

7: Kim KA, Park JY. Pharmacokinetic comparisons of bepotastine besilate and
bepotastine salicylate in healthy subjects. Clin Drug Investig. 2013
Dec;33(12):913-9. doi: 10.1007/s40261-013-0140-7. PubMed PMID: 24105252.

8: Carr WW, Nayak AS, Ratner PH, Gow JA, McNamara TR, Williams JI; Bepotastine
Besilate Ophthalmic Solution 1.5% (Bepreve) Study Group. Efficacy of bepotastine
besilate ophthalmic solution 1.5% for seasonal allergic conjunctivitis: a
randomized, placebo-controlled, natural exposure, clinical trial. Allergy Asthma
Proc. 2013 May-Jun;34(3):247-54. PubMed PMID: 23484763.

9: McCabe CF, McCabe SE. Comparative efficacy of bepotastine besilate 1.5%
ophthalmic solution versus olopatadine hydrochloride 0.2% ophthalmic solution
evaluated by patient preference. Clin Ophthalmol. 2012;6:1731-8. doi:
10.2147/OPTH.S35431. Epub 2012 Oct 29. PubMed PMID: 23152650; PubMed Central
PMCID: PMC3497448.

10: Meier EJ, Torkildsen GL, Gow JA, McNamara TR, Gomes PJ, Williams JI;
Bepotastine Besilate Ophthalmic Solutions Study Group. Integrated phase III
trials of bepotastine besilate ophthalmic solution 1.5% for ocular itching
associated with allergic conjunctivitis. Allergy Asthma Proc. 2012
May-Jun;33(3):265-74. PubMed PMID: 22991696.

11: Cho KH, Choi HG. Development of novel bepotastine salicylate salt
bioequivalent to the commercial bepotastine besilate in beagle dogs. Drug Dev Ind
Pharm. 2013 Jun;39(6):901-8. doi: 10.3109/03639045.2012.717295. Epub 2012 Sep 10.
PubMed PMID: 22963365.

12: Tanizaki H, Ikoma A, Fukuoka M, Miyachi Y, Kabashima K. Effects of
bepotastine and fexofenadine on histamine-induced flare, wheal and itch. Int Arch
Allergy Immunol. 2012;158(2):191-5. doi: 10.1159/000330663. Epub 2012 Jan 26.
PubMed PMID: 22286689.

13: Kawakami T, Kimura S, Haga T, Doi R, Kyoya M, Nakagawa K, Soma Y.
Health-related quality of life assessed by the effect of bepotastine besilate in
patients with pruritus: importance of emotions score in atopic dermatitis. J
Dermatol. 2012 Jun;39(6):527-30. doi: 10.1111/j.1346-8138.2011.01418.x. Epub 2011
Oct 31. PubMed PMID: 22035542.

14: Williams JI, Kennedy KS, Gow JA, Torkildsen GL, Abelson MB, Gomes PJ,
McNamara TR; Bepotastine Besilate Ophthalmic Solutions Study Group. Prolonged
effectiveness of bepotastine besilate ophthalmic solution for the treatment of
ocular symptoms of allergic conjunctivitis. J Ocul Pharmacol Ther. 2011
Aug;27(4):385-93. doi: 10.1089/jop.2011.0005. Epub 2011 Jun 7. PubMed PMID:

15: Wingard JB, Mah FS. Critical appraisal of bepotastine in the treatment of
ocular itching associated with allergic conjunctivitis. Clin Ophthalmol.
2011;5:201-7. doi: 10.2147/OPTH.S8665. Epub 2011 Feb 15. PubMed PMID: 21386912;
PubMed Central PMCID: PMC3046989.

16: Zhang D, Tashiro M, Shibuya K, Okamura N, Funaki Y, Yoshikawa T, Kato M,
Yanai K. Next-day residual sedative effect after nighttime administration of an
over-the-counter antihistamine sleep aid, diphenhydramine, measured by positron
emission tomography. J Clin Psychopharmacol. 2010 Dec;30(6):694-701. PubMed PMID:

17: Hashimoto T, Ishii N, Hamada T, Dainichi T, Karashima T, Nakama T, Yasumoto
S. Effects of olopatadine hydrochloride, a histamine h(1) receptor antagonist, on
histamine-induced skin responses. Dermatol Res Pract. 2010;2010. pii: 638051.
doi: 10.1155/2010/638051. Epub 2010 Sep 16. PubMed PMID: 20886023; PubMed Central
PMCID: PMC2945667.

18: Williams JI, Gow JA, Klier SM, McCue SL, Salapatek AM, McNamara TR.
Non-clinical pharmacology, pharmacokinetics, and safety findings for the
antihistamine bepotastine besilate. Curr Med Res Opin. 2010 Oct;26(10):2329-38.
doi: 10.1185/03007995.2010.486753. Review. PubMed PMID: 20735291.

19: Lyseng-Williamson KA. Oral bepotastine: in allergic disorders. Drugs. 2010
Aug 20;70(12):1579-91. doi: 10.2165/11205880-000000000-00000. Review. Erratum in:
Drugs. 2011 Apr 16;71(6):756. PubMed PMID: 20687621.

20: Torkildsen GL, Williams JI, Gow JA, Gomes PJ, Abelson MB, McNamara TR;
Bepotastine Besilate Ophthalmic Solutions Clinical Study Group. Bepotastine
besilate ophthalmic solution for the relief of nonocular symptoms provoked by
conjunctival allergen challenge. Ann Allergy Asthma Immunol. 2010
Jul;105(1):57-64. doi: 10.1016/j.anai.2010.04.005. PubMed PMID: 20642205.