Alcaftadine, a new antihistamine with combined antagonist activity at histamine H₁, H₂, and H₄ receptors

References

• Jutel M, Akdis M, Akdis CA. Histamine, histamine receptors and their role in immune pathology. Clin Exp Allergy. 2009;39(12):1786–1800.
   Web of Science ®Google Scholar
• Huang J-F, Thurmond R. The new biology of histamine receptors. Curr Allergy Asthma Rep. 2008;8(1):21–27.
   Web of Science ®Google Scholar
• Ono SJ, Abelson MB. Allergic conjunctivitis: update on pathophysiology and prospects for future treatment. J Allergy Clin Immunol. 2005;115(1):118–122.
   PubMed Web of Science ®Google Scholar
• Leonardi A. Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005;10(3):505–520.
   PubMedGoogle Scholar
• Leonardi A, De Dominicis C, Motterle L. Immunopathogenesis of ocular allergy: a schematic approach to different clinical entities. Curr Opin Allergy Clin Immunol. 2007;7(5):429–435.
   PubMed Web of Science ®Google Scholar
• Abramowicz M, editor. Drugs for allergic disorders. Medical Letter Treatment Guidelines. 2010;8:9–18.
   Google Scholar
• Greiner JV Edwards-Swanson K, Ingerman A. Evaluation of alcaftadine 0.25% ophthalmic solution in acute allergic conjunctivitis at 15 minutes and 16 hours after instillation versus placebo and olopatadine 0.1%. Clin Ophthalmol. 2011;5:87–93.
   PubMedGoogle Scholar
• Torkildsen G, Shedden A. The safety and efficacy of alcaftadine 0.25% ophthalmic solution for the prevention of itching associated with allergic conjunctivitis. Curr Med Res Opin. 2011;27(3):623–631.
   PubMed Web of Science ®Google Scholar
• Bohets H, McGowan C, Mannens G, Schroeder N, Edwards-Swanson K, Shapiro A. Clinical pharmacology of alcaftadine, a novel antihistamine for the prevention of allergic conjunctivitis. J Ocul Pharmacol Ther. 2011;27(2):187–195.
   Web of Science ®Google Scholar
• Janssens F, Diels G, Leenaerts J, inventors; Imidaz[2,1-b]benzazepine derivatives, compositions and method of use, 1995. United States Patent US5468743.
   Google Scholar
• Awouters F, Vermeire J, Smeyers F, Vermote P, Van Beck R, Niemegeers CJE. Oral antiallergic activity in Ascaris hypersensitive dogs: a study of known antihistamines and of the new compounds ramastine (R 57 959) and levocabastine (R 50 547). Drug Dev Res. 1986;8(1–4):95–102.
   Web of Science ®Google Scholar
• Tagari P, Black C, Marshall S, Ford-Hutchinson AW. A rapid biochemical method for measuring antigen-induced pulmonary eosinophil margination in allergic guinea pigs. J Immunol Methods. 1993;163(1):49–58.
   Web of Science ®Google Scholar
• Smit MJ, Timmerman H, Hijzelendoorn JC, Fukui H, Leurs R. Regulation of the human histamine H1 receptor stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 1996;117(6):1071–1080.
   Web of Science ®Google Scholar
• Leurs R, Smit MJ, Menge WM, Timmerman H. Pharmacological characterization of the human histamine H2 receptor stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 1994;112(3):847–854.
   PubMed Web of Science ®Google Scholar
• Thurmond RL, Desai PJ, Dunford PJ, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol⁴ Exp Ther. 2004;309(1):404–413.
   PubMed Web of Science ®Google Scholar
• Cheng Y-C, Prusoff WH. Relation between the inhibition constant K1 and the concentration of inhibitor which causes fifty per cent inhibition (I50) of an enzymic reaction. Biochem Pharmacol. 1973;22(23):3099–3108.
   PubMed Web of Science ®Google Scholar
• Sharif NA, Xu SX, Miller ST, Gamache DA, Yanni JM. Characterization of the ocular antiallergic and antihistaminic effects of olopatadine (AL-4943A), a novel drug for treating ocular allergic diseases. J Pharmacol Exp Ther. 1996;278(3):1252–1261.
   PubMed Web of Science ®Google Scholar
• Cowden JM, Zhang M, Dunford PJ, Thurmond RL. The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation. J Invest Dermatol. 2010;130(4):1023–1033.
   Web of Science ®Google Scholar
• Dunford PJ, O’Donnell N, Riley JP, Williams KN, Karlsson L, Thurmond RL. The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells. J Immunol. 2006;176(11):7062–7070.
   Web of Science ®Google Scholar
• Ling P, Ngo K, Nguyen S, et al. Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol. 2004;142(1):161–171.
   PubMed Web of Science ®Google Scholar
• Simons FE, Simons KJ. Histamine and Hl-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2011;128(6):1139–1150.
   PubMed Web of Science ®Google Scholar
• Gelfand EW, Appajosyula S, Meeves S. Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research. Curr Med Res Opin. 2004;20(1):73–81.
   PubMed Web of Science ®Google Scholar
• Abelson MB, Udell IJ. H2-receptors in the human ocular surface. Arch Ophthalmol. 1981;99(2):302–304.
   PubMedGoogle Scholar
• Woodward DF, Johnson L, Spada C, Chen J. Effect of cimetidine and pyrilamine on histamine-induced ocular surface hyperemia. J Ocul Pharmacol. 1986;2(3):275–278.
   Google Scholar
• Nakano Y, Takahashi Y, Ono R, Kurata Y, Kagawa Y, Kamei C. Role of histamine H4 receptor in allergic conjunctivitis in mice. Eur J Pharmacol. 2009;608(1–3):71–75.
   Web of Science ®Google Scholar
• Zampeli E, Thurmond RL, Tiligada E. The histamine H4 receptor antagonist JNJ7777120 induces increases in the histamine content of the rat conjunctiva. Inflamm Res. 2009;58(6):285–291.
   Web of Science ®Google Scholar
• Canonica GW, Ciprandi G. Antiallergic drugs and the immune response. Interactions and possible clinical relevance. Allergy. 1989;44(1):1–5.
   Web of Science ®Google Scholar
• Clark RAF, Sandler JA, Gallin JI, Kaplan AP. Histamine modulation of eosinophil migration. J Immunol. 1977;118(1):137–145.
   Web of Science ®Google Scholar
• Reher TM, Neumann D, Buschauer A, Seifert R. Incomplete activation of human eosinophils via the histamine H4-receptor: evidence for ligand-specific receptor conformations. Biochem Pharmacol. 2012;84(2):192–203.
   Web of Science ®Google Scholar
• Woodward DF, Spada CS, Hawley SB, Nieves AL. Conjunctival eosinophil infiltration evoked by histamine and immediate hypersensitivity. Modification by H1- and H2-receptor blockade. Invest Ophthalmol Vis Sci. 1986;27(10):1495–1503.
   Web of Science ®Google Scholar
• Leonardi A, Di Stefano A, Vicari C, Motterle L, Brun P. Histamine H4 receptors in normal conjunctiva and in vernal keratoconjunctivitis. Allergy. 2011;66(10):1360–1366.
   PubMed Web of Science ®Google Scholar
• Takahashi Y, Kagawa Y, Izawa K, Ono R, Akagi M, Kamei C. Effect of histamine H4 receptor antagonist on allergic rhinitis in mice. Int Immunopharmacol. 2009;9(6):734–738.
   Web of Science ®Google Scholar
• Ono SJ, Lane K. Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis. Drug Des Devel Ther. 2011;5:77–84.
   PubMed Web of Science ®Google Scholar
• Offiah I, Calder VL. Immune mechanisms in allergic eye diseases: what is new? Curr Opin Allergy Clin Immunol. 2009;9(5):477–481.
   Web of Science ®Google Scholar