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Review

Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate

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Pages 2329-2338 | Accepted 15 Apr 2010, Published online: 25 Aug 2010

References

  • Baba S, Sakakura Y, Iwata S, et al. Early phase II study of TAU-284 (betotastine besilate) on perennial allergic rhinitis [in Japanese]. J Clin Ther Med 1997;13:1217-35
  • Baba S, Takasaki T, Baba K, et al. Late phase II clinical stuffy of TAU-284 for perennial allergic rhinitis – dose finding study by the double-blind method [in Japanese]. J Clin Ther Med 1997;13:1259-86
  • Baba S, Takasaki T, Baba K, et al. Long-term treatment of TAU-284 (betotastine besilate) on perennial allergic rhinitis [in Japanese]. J Clin Ther Med 1997;13:1361-82
  • Baba S. Post-marketing surveillance study of Talion tablets on pediatric allergic rhinitis [in Japanese]. Rinsho Igaku 2002;18:1371-87
  • Maruta H, Nagata M, Koga H, et al. Clinical evaluation of bepotastine besilate (Talion tablets) on chronic urticaria [in Japanese]. J New Rem Clin 2004;53:576-82
  • Ishibashi Y, Harada S, Niimura M, et al. Late phase II study of TAU-284 (betotastine besilate) on chronic urticaria – optimal dose finding study by double-blind technique [in Japanese]. J Clin Ther Med 1997;13:1237-57
  • Ishibashi Y, Harada S, Niimura M, et al. Long-term treatment of TAU-284 (betotastine besilate) on chronic urticaria [in Japanese]. J Clin Ther Med 1997;13:1337-59
  • Kawashima M, Harada S, Kawashima M. Phase III study of TAU-284 (bepotastine besilate) on chronic urticaria. A multicenter double blind comparative study with placebo [in Japanese]. J Clin Ther Med 2002;18:501-19
  • Talion [package insert]. Osaka, Japan: Mitsubishi Tanabe Pharmaceutical Co; 2007
  • Kato M, Nishida A, Aga Y, et al. Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel anti-allergic agent betotastine besilate. Arzneimittelforschung 1997;47:1116-24
  • Yato N, Murata T, Saito N, et al. Antiallergic activity of betotastine besilate (TAU-284), a new antiallergic drug [in Japanese]. Nippon Yakurigaku Zasshi - Folia Pharmacologica Japonica 1997;110:19-29
  • Bepreve 1.5% [package insert]. Irvine, CA: ISTA Pharmaceuticals; 2009
  • Dykewicz MS, Fineman S, Skoner DP, et al. Diagnosis and management of rhinitis: complete guidelines of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology. American Academy of Allergy, Asthma, and Immunology. Ann Allergy Asthma Immunol 1998;81:478-518
  • Raizman M. Results of a survey of patients with ocular allergy treated with topical ketorolac tromethamine. Clin Ther 1995;17:882-90
  • Berger W, Abelson MB, Gomes PJ, et al. Effects of adjuvant therapy with 0.1% olopatadine hydrochloride ophthalmic solution on quality of life in patients with allergic rhinitis using systemic or nasal therapy. Ann Allergy Asthma Immunol 2005;95:361-71
  • Kaliner MA. Azelastine and olopatadine in the treatment of allergic rhinitis. Ann Allergy Asthma Immunol 2009;103:373-80
  • Abelson MB, Smith L, Chapin M. Ocular allergic disease: mechanisms, disease sub-types, treatment. Ocul Surf 2003;1:38-60
  • Izumi N, Mizuguchi H, Umehara H, et al. Analysis of disease-dependent sedative profiles of H1-antihistamines by large scale surveillance using the visual analog scale. Methods Find Exp Clin Pharmacol 2008;30:225-30
  • Bousquet J, Van Cauwenberge P, Bachert C, et al. Requirements for medications commonly used in the treatment of allergic rhinitis. European Academy of Allergy and Clinical Immunology (EAACI), Allergic Rhinitis and its Impact on Asthma (ARIA). Allergy 2003;58:192-7
  • Yanai K, Tashiro M, Okamura N. Non-sedating second-generation antihistamines: The penetration through blood-brain barrier measured by PET [in Japanese]. Nishinihon J Dermatol 2009;71:3-6
  • Honda H. Inhibitory effect of betotastine on anaphylactic and histamine-antagonizing reactions in guinea pigs [in Japanese]. Jpn Pharmacol Ther 1997;25:9-18
  • Yang TQ, Takeuchi K, Hayashi S, et al. Effect of histamine on the permeability of the nasal mucosa in vivo [in Japanese]. Acta Oto-Laryngol 2003; 123:401-5
  • Yamaguchi Y, Hayashi Y, Sugama Y, et al. Highly purified murine interleukin 5 (IL-5) stimulates eosinophil function and prolongs in vitro survival. IL-5 as an eosinophil chemotactic factor. J Exp Med 1988;167:1737-42
  • Kaminuma O, Ogawa K, Kikkawa H, et al. A novel antiallergic drug, betotastine besilate, suppresses interleukin-5 production by human peripheral blood mononuclear cells. Biol Pharm Bull 1998;21:411-3
  • Higuchi H, Hara M, Yamamoto K, et al. Mast cells play a critical role in the pathogenesis of viral myocarditis. Circulation 2008;118:363-72
  • Kitaba S, Murota H, Yahata Y, et al. Novel functional aspect of antihistamines: the impact of bepotastine besilate on substance P-induced events [in Japanese]. J Allergy. 2009, Article ID 853687. doi:10.1155/2009/853687
  • Tanizaki H, Kambe N, Nakamura Y, et al. Oral administration of bepotastine besilate suppressed scratching behavior of atopic dermatitis model NC/Nga mice. Int Arch Allergy Immunol 2008;145:277-82
  • Andoh T, Kuraishi Y. Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice. Eur J Pharmacol 2006;547:59-64
  • Murata T, Matsumoto Y, Suzuki T, et al. Effect of betotastine besilate (TAU-284), a novel antiallergic agent, on experimental allergic rhinitis [in Japanese]. Arerugi 1997;46:576-84
  • Kobayashi M, Kabashima K, Nakamura M, et al. Downmodulatory effects of the antihistaminic drug bepotastine on cytokine/chemokine production and CD54 expression in human keratinocytes. Skin Pharmacol Physiol 2009;22:45-8
  • Tokura Y, Kobayashi M, Kabashima K. Epidermal chemokines and modulation by antihistamines, antibiotics and antifungals. Exp Dermatol 2008;17:81-90
  • Ueno M, Inagaki N, Nagai H, et al. Anti-allergic action of betotastine besilate (TAU-284) in animal models: A comparison with ketotifen. Pharmacology 1998;57:206-14
  • Sakai A, Kikuchi M, Yato N, et al. Inhibitory effect of betotastine besilate on antigen-induced airway eosinophil infiltration and peripheral blood eosinophilia in mice. Arzneimittelforschung 1997;47:954-8
  • Creticos PS, Peters SP, Adkinson NF Jr, et al. Peptide leukotriene release after antigen challenge in patients sensitive to ragweed. N Engl J Med. 1984;310:1626-30
  • Sato S, Bae S, Ogawa F. Bepotastine besilate suppresses expression of ICAM-1 in the endothelial cell [in Japanese]. Jap J Clin Exp Med 2006;83:1245-8
  • Sato S, Saito E, Takehara K. Inhibitory effect of bepotastine besilate on skin contact hypersensitivity reactions, which are type IV allergies [in Japanese]. Jap J Clin Exp Med 2003;80:377-9
  • Matsubara S, Ono C, Yamazaki N, et al. Effect of betotastine besilate (TAU-284) on experimental asthma model in guinea pigs [in Japanese]. Jpn Pharmacol Ther 1997;25:901-6
  • Sakamoto O, Okanari E, Ueno H. The inhibition action of betotastine besilate (TAU-284), a novel anti-allergy drug, on experimental guinea pig bronchoconstriction reactions [in Japanese]. Jpn Pharmacol Ther 1997;25:889-94
  • Matsubara S, Ono C, Yamazaki N, et al. Inhibitory effects of betotastine, a novel antiallergic drug, on histamine-induced bronchoconstriction in anesthetized dogs [in Japanese]. Jpn Pharmacol Ther 1997;25:25-30
  • Simons FER. Advances in H1-antihistamines. N Eng J Med 2004;351:2203-17
  • Ohashi R, Kamikozawa Y, Sugiura M, et al. Effect of P-glycoprotein on intestinal absorption and brain penetration of anti-allergic agent bepotastine besilate. Drug Metab Dispos 2006;34:793-9
  • Hishinuma S, Sato Y, Kobayashi Y, et al. Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci 2008;107:66-79
  • Narita H, Kikuchi M, Asahi T, et al. General pharmacology of betotastine besilate (TAU-284), a novel anti-allergic agent [in Japanese]. Jpn Pharmacol Ther 1997;25:907-24
  • Tanaka H, Nishimaru K, Sekine T, et al. Effects of terfenadine, betotastine and ketotifen on the action potential and membrane currents in isolated guinea-pig myocardium. Res Comm Pharm Tox 1997;2:163-74
  • Ohashi R, Tsukimoto M, Nakamura S, et al. Pharmacokinetic studies of bepotastine besilate (TAU-284) (I): Absorption, distribution, metabolism, and excretion in rats and dogs receiving a single oral dose [in Japanese]. Xenobio Metab Dispos 1997;12:417-38
  • Tsukimoto M, Ohashi R, Nakamura S, et al. Study (II) relating to the internal pharmacokinetics of betotastine besilate (TAU-284): transfer into the fetus and into milk in rats, and distribution and excretion during repeated administration [in Japanese]. Xenobio Metab Dispos 1997;12:439-59
  • Koguchi A, Kawai Y, Suetake K, et al. 4-week and 26-week repeated administration toxicity studies of betotastine besilate in rats [in Japanese]. Pharmacometrics 1997;53:299-318
  • Koguchi A, Kawai Y, Ichiki T, et al. 4-week and 26-week repeated administration toxicity studies of betotastine besilate in dogs [in Japanese]. Pharmacometrics 1997;53:319-26
  • Nishida A, Asano Y, Hori M, et al. Reproductive toxicity studies of betotastine besilate in rats and rabbits [in Japanese]. Pharmacometrics 1997;53:327-49

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