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Chemical Compound Review

Accolate     cyclopentyl N-[3-[[2-methoxy-4-[(2...

Synonyms: Accoleit, Aeronix, Olmoran, Zafirst, Respix, ...
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Disease relevance of zafirlukast


Psychiatry related information on zafirlukast


High impact information on zafirlukast


Chemical compound and disease context of zafirlukast


Biological context of zafirlukast

  • BACKGROUND: Single doses of zafirlukast attenuate exercise-induced bronchoconstriction (EIB), but previous studies have not measured zafirlukast's effects after regular dosing or its duration of effect beyond 4 hours [16].
  • Compared with placebo, zafirlukast produced a significant improvement over baseline in the primary study endpoint of mean morning peak expiratory flow rate (PEFR) (18.7 L/min versus 1.5 L/min, p < 0.001), as well as in evening PEFR (p < 0.01), FEV(1) (p < 0.05), daytime symptom score (p < 0.001), and beta(2)-agonist use (p < 0.001) [17].
  • On repeat LTE 4 inhalation challenge after 6 weeks, zafirlukast treatment prevented further airway eosinophilia and decrease in FEV 1 seen in the placebo group [10].
  • The combination of zafirlukast and loratadine reduced the AUC FEV1 during EAR and LAR further, by 75 +/- 8% and 74 +/- 14%, respectively (p < 0.05 versus control) [18].
  • By means of heterologous dissociation time courses, we demonstrated that zafirlukast, iralukast, and BAY u9773 selectively competed only for (3)H-LTD(4) binding sites, whereas pobilukast, pranlukast, and CGP 57698 dissociated both (3)H-LTC(4) and (3)H-LTD(4) from their binding sites [19].

Anatomical context of zafirlukast


Associations of zafirlukast with other chemical compounds


Gene context of zafirlukast


Analytical, diagnostic and therapeutic context of zafirlukast

  • Severe liver injury after treatment with the leukotriene receptor antagonist zafirlukast [3].
  • Eighteen normal male subjects were recruited for a double-blind, placebo-controlled, randomized, two-period crossover study to determine the effects of a new, potent, highly selective, oral peptide leukotriene antagonist (ICI 204,219) on cutaneous vasculature [33].
  • In multicenter trials in patients with chronic, stable asthma, zafirlukast reduced asthma symptoms, decreased as-needed beta-agonist use, and improved pulmonary function without increasing the number of adverse events [5].
  • The effect of zafirlukast (Z) to alter the inflammatory response to segmental antigen challenge (SAC) was assessed by bronchoalveolar lavage (BAL) in this double-blind, placebo-controlled, two-period, crossover trial in 11 allergic asthmatic patients [34].
  • The overall treatment failure rate was significantly lower in the zafirlukast group compared with the placebo group (P <.003) [35].


  1. Zafirlukast and Churg-Strauss syndrome. Katz, R.S., Papernik, M. JAMA (1998) [Pubmed]
  2. Pulmonary infiltrates, eosinophilia, and cardiomyopathy following corticosteroid withdrawal in patients with asthma receiving zafirlukast. Wechsler, M.E., Garpestad, E., Flier, S.R., Kocher, O., Weiland, D.A., Polito, A.J., Klinek, M.M., Bigby, T.D., Wong, G.A., Helmers, R.A., Drazen, J.M. JAMA (1998) [Pubmed]
  3. Severe liver injury after treatment with the leukotriene receptor antagonist zafirlukast. Reinus, J.F., Persky, S., Burkiewicz, J.S., Quan, D., Bass, N.M., Davern, T.J. Ann. Intern. Med. (2000) [Pubmed]
  4. The addition of zafirlukast to cetirizine improves the treatment of chronic urticaria in patients with positive autologous serum skin test results. Bagenstose, S.E., Levin, L., Bernstein, J.A. J. Allergy Clin. Immunol. (2004) [Pubmed]
  5. Summary of clinical trials with zafirlukast. Calhoun, W.J. Am. J. Respir. Crit. Care Med. (1998) [Pubmed]
  6. Zafirlukast. A review of its pharmacology and therapeutic potential in the management of asthma. Adkins, J.C., Brogden, R.N. Drugs (1998) [Pubmed]
  7. Role of cysteinyl leukotrienes in nociceptive and inflammatory conditions in experimental animals. Jain, N.K., Kulkarni, S.K., Singh, A. Eur. J. Pharmacol. (2001) [Pubmed]
  8. Lung function improvement in asthma with a cysteinyl-leukotriene receptor antagonist. Hui, K.P., Barnes, N.C. Lancet (1991) [Pubmed]
  9. New approaches to anti-inflammatory therapy for asthma. Wenzel, S.E. Am. J. Med. (1998) [Pubmed]
  10. Leukotriene E(4)-induced persistent eosinophilia and airway obstruction are reversed by zafirlukast in patients with asthma. Laitinen, A., Lindqvist, A., Halme, M., Altraja, A., Laitinen, L.A. J. Allergy Clin. Immunol. (2005) [Pubmed]
  11. Churg-Strauss syndrome after zafirlukast in two patients not receiving systemic steroid treatment. Green, R.L., Vayonis, A.G. Lancet (1999) [Pubmed]
  12. Inhibition of 5-lipoxygenase diminishes neurally evoked tachykinergic contraction of guinea pig isolated airway. McAlexander, M.A., Myers, A.C., Undem, B.J. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  13. Montelukast in the prophylaxis of migraine: a potential role for leukotriene modifiers. Sheftell, F., Rapoport, A., Weeks, R., Walker, B., Gammerman, I., Baskin, S. Headache. (2000) [Pubmed]
  14. Treatment of acquired cold urticaria with cetirizine and zafirlukast in combination. Bonadonna, P., Lombardi, C., Senna, G., Canonica, G.W., Passalacqua, G. J. Am. Acad. Dermatol. (2003) [Pubmed]
  15. Failure of zafirlukast to prevent ibuprofen-induced anaphylaxis. Menendez, R., Venzor, J., Ortiz, G. Ann. Allergy Asthma Immunol. (1998) [Pubmed]
  16. The effect of zafirlukast on repetitive exercise-induced bronchoconstriction: the possible role of leukotrienes in exercise-induced refractoriness. Dessanges, J.F., Préfaut, C., Taytard, A., Matran, R., Naya, I., Compagnon, A., Dinh-Xuan, A.T. J. Allergy Clin. Immunol. (1999) [Pubmed]
  17. Zafirlukast improves asthma control in patients receiving high-dose inhaled corticosteroids. Virchow, J.C., Prasse, A., Naya, I., Summerton, L., Harris, A. Am. J. Respir. Crit. Care Med. (2000) [Pubmed]
  18. Combined antagonism of leukotrienes and histamine produces predominant inhibition of allergen-induced early and late phase airway obstruction in asthmatics. Roquet, A., Dahlén, B., Kumlin, M., Ihre, E., Anstrén, G., Binks, S., Dahlén, S.E. Am. J. Respir. Crit. Care Med. (1997) [Pubmed]
  19. A kinetic binding study to evaluate the pharmacological profile of a specific leukotriene C(4) binding site not coupled to contraction in human lung parenchyma. Ravasi, S., Capra, V., Mezzetti, M., Nicosia, S., Rovati, G.E. Mol. Pharmacol. (2000) [Pubmed]
  20. Expression of functional cysteinyl leukotriene receptors by human basophils. Gauvreau, G.M., Plitt, J.R., Baatjes, A., MacGlashan, D.W. J. Allergy Clin. Immunol. (2005) [Pubmed]
  21. Variant LTC(4) synthase allele modifies cysteinyl leukotriene synthesis in eosinophils and predicts clinical response to zafirlukast. Sampson, A.P., Siddiqui, S., Buchanan, D., Howarth, P.H., Holgate, S.T., Holloway, J.W., Sayers, I. Thorax (2000) [Pubmed]
  22. An examination of the influence of the epithelium on contractile responses to peptidoleukotrienes and blockade by ICI 204,219 in isolated guinea pig trachea and human intralobar airways. Buckner, C.K., Fedyna, J.S., Robertson, J.L., Will, J.A., England, D.M., Krell, R.D., Saban, R. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  23. Zafirlukast metabolism by cytochrome P450 3A4 produces an electrophilic alpha,beta-unsaturated iminium species that results in the selective mechanism-based inactivation of the enzyme. Kassahun, K., Skordos, K., McIntosh, I., Slaughter, D., Doss, G.A., Baillie, T.A., Yost, G.S. Chem. Res. Toxicol. (2005) [Pubmed]
  24. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Sarau, H.M., Ames, R.S., Chambers, J., Ellis, C., Elshourbagy, N., Foley, J.J., Schmidt, D.B., Muccitelli, R.M., Jenkins, O., Murdock, P.R., Herrity, N.C., Halsey, W., Sathe, G., Muir, A.I., Nuthulaganti, P., Dytko, G.M., Buckley, P.T., Wilson, S., Bergsma, D.J., Hay, D.W. Mol. Pharmacol. (1999) [Pubmed]
  25. Inhibition of leukotriene D4-induced bronchoconstriction in subjects with asthma: a concentration-effect study of ICI 204,219. Smith, L.J., Glass, M., Minkwitz, M.C. Clin. Pharmacol. Ther. (1993) [Pubmed]
  26. Comparison of inhaled salmeterol and oral zafirlukast in patients with asthma. Busse, W., Nelson, H., Wolfe, J., Kalberg, C., Yancey, S.W., Rickard, K.A. J. Allergy Clin. Immunol. (1999) [Pubmed]
  27. Influence of zafirlukast and loratadine on exercise-induced bronchoconstriction. Dahlén, B., Roquet, A., Inman, M.D., Karlsson, O., Naya, I., Anstrén, G., O'Byrne, P.M., Dahlén, S.E. J. Allergy Clin. Immunol. (2002) [Pubmed]
  28. Inhaled fluticasone propionate: a review of its therapeutic efficacy at dosages < or = 500 microg/day in adults and adolescents with mild to moderate asthma. Jarvis, B., Faulds, D. Drugs (1999) [Pubmed]
  29. Pharmacokinetic profile of zafirlukast. Dekhuijzen, P.N., Koopmans, P.P. Clinical pharmacokinetics. (2002) [Pubmed]
  30. Pioglitazone is metabolised by CYP2C8 and CYP3A4 in vitro: potential for interactions with CYP2C8 inhibitors. Jaakkola, T., Laitila, J., Neuvonen, P.J., Backman, J.T. Basic & clinical pharmacology & toxicology. (2006) [Pubmed]
  31. Inhibition of human cytochrome P450 isoforms in vitro by zafirlukast. Shader, R.I., Granda, B.W., von Moltke, L.L., Giancarlo, G.M., Greenblatt, D.J. Biopharmaceutics & drug disposition. (1999) [Pubmed]
  32. Clinical pharmacology of leukotriene receptor antagonists and 5-lipoxygenase inhibitors. Drazen, J. Am. J. Respir. Crit. Care Med. (1998) [Pubmed]
  33. The effect of the oral leukotriene antagonist, ICI 204,219, on leukotriene D4 and histamine-induced cutaneous vascular reactions in man. Bernstein, J.A., Greenberger, P.A., Patterson, R., Glass, M., Krell, R., Thyrum, P.T. J. Allergy Clin. Immunol. (1991) [Pubmed]
  34. Effect of zafirlukast (Accolate) on cellular mediators of inflammation: bronchoalveolar lavage fluid findings after segmental antigen challenge. Calhoun, W.J., Lavins, B.J., Minkwitz, M.C., Evans, R., Gleich, G.J., Cohn, J. Am. J. Respir. Crit. Care Med. (1998) [Pubmed]
  35. An evaluation of zafirlukast in the treatment of asthma with exploratory subset analyses. Tashkin, D.P., Nathan, R.A., Howland, W.C., Minkwitz, M.C., Simonson, S.G., Bonuccelli, C.M. J. Allergy Clin. Immunol. (1999) [Pubmed]
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