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Chemical Compound Review

SureCN4487     2-[1-[[(1R)-1-[3-[2-(7- chloroquinolin-2...

Synonyms: AC1L1U7X
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Disease relevance of montelukast


High impact information on montelukast


Chemical compound and disease context of montelukast


Biological context of montelukast


Anatomical context of montelukast


Associations of montelukast with other chemical compounds

  • No apparent affinity binding for the receptors was detected for the CysLT1-selective antagonists montelukast and zafirlukast [23].
  • In summary, treatment of the two main components of asthma (inflammation and bronchoconstriction) with fluticasone propionate and salmeterol in a combination product was a more effective initial maintenance treatment strategy than treatment with montelukast, a single-mediator antagonist [24].
  • METHODS: Ten adults with mild-to-moderate atopic asthma participated in a randomized, 4-way crossover study design comparing placebo, 5 mg of desloratadine, 10 mg of montelukast, and the combination administered at 26 hours and 2 hours before each allergen challenge conducted at least 7 days apart [25].
  • Methods and Measurements: In a randomized, placebo-controlled, crossover study of 192 subjects with moderate asthma, we compared the clinical efficacy of regular treatment over 14 weeks with the combination of montelukast and salmeterol to that with the combination of beclomethasone and salmeterol in moderate asthma [26].
  • Triamcinolone was better than placebo or montelukast for effects on all other surrogate inflammatory markers (P <.05), including exhaled nitric oxide, blood eosinophils, serum eosinophil cationic protein, plasma intracellular circulating adhesion molecule 1, and plasma E-selectin [27].

Gene context of montelukast


Analytical, diagnostic and therapeutic context of montelukast


  1. Montelukast, a leukotriene-receptor antagonist, for the treatment of mild asthma and exercise-induced bronchoconstriction. Leff, J.A., Busse, W.W., Pearlman, D., Bronsky, E.A., Kemp, J., Hendeles, L., Dockhorn, R., Kundu, S., Zhang, J., Seidenberg, B.C., Reiss, T.F. N. Engl. J. Med. (1998) [Pubmed]
  2. Marked peripheral edema associated with montelukast and prednisone. Geller, M. Ann. Intern. Med. (2000) [Pubmed]
  3. Montelukast, a once-daily leukotriene receptor antagonist, in the treatment of chronic asthma: a multicenter, randomized, double-blind trial. Montelukast Clinical Research Study Group. Reiss, T.F., Chervinsky, P., Dockhorn, R.J., Shingo, S., Seidenberg, B., Edwards, T.B. Arch. Intern. Med. (1998) [Pubmed]
  4. The leukotriene receptor antagonist montelukast in the treatment of chronic idiopathic urticaria: a single-blind, placebo-controlled, crossover clinical study. Erbagci, Z. J. Allergy Clin. Immunol. (2002) [Pubmed]
  5. Concomitant montelukast and loratadine as treatment for seasonal allergic rhinitis: a randomized, placebo-controlled clinical trial. Meltzer, E.O., Malmstrom, K., Lu, S., Prenner, B.M., Wei, L.X., Weinstein, S.F., Wolfe, J.D., Reiss, T.F. J. Allergy Clin. Immunol. (2000) [Pubmed]
  6. Oral montelukast compared with inhaled salmeterol to prevent exercise-induced bronchoconstriction. A randomized, double-blind trial. Exercise Study Group. Edelman, J.M., Turpin, J.A., Bronsky, E.A., Grossman, J., Kemp, J.P., Ghannam, A.F., DeLucca, P.T., Gormley, G.J., Pearlman, D.S. Ann. Intern. Med. (2000) [Pubmed]
  7. Up-regulation of cysteinyl leukotriene 1 receptor by IL-13 enables human lung fibroblasts to respond to leukotriene C4 and produce eotaxin. Chibana, K., Ishii, Y., Asakura, T., Fukuda, T. J. Immunol. (2003) [Pubmed]
  8. Lipoxin A4 stimulates a cytosolic Ca2+ increase in human bronchial epithelium. Bonnans, C., Mainprice, B., Chanez, P., Bousquet, J., Urbach, V. J. Biol. Chem. (2003) [Pubmed]
  9. Eosinophilic oesophagitis: a novel treatment using Montelukast. Attwood, S.E., Lewis, C.J., Bronder, C.S., Morris, C.D., Armstrong, G.R., Whittam, J. Gut (2003) [Pubmed]
  10. Effects of montelukast and budesonide on airway responses and airway inflammation in asthma. Leigh, R., Vethanayagam, D., Yoshida, M., Watson, R.M., Rerecich, T., Inman, M.D., O'Byrne, P.M. Am. J. Respir. Crit. Care Med. (2002) [Pubmed]
  11. Reversal of Allergen-induced Airway Remodeling by CysLT1 Receptor Blockade. Henderson, W.R., Chiang, G.K., Tien, Y.T., Chi, E.Y. Am. J. Respir. Crit. Care Med. (2006) [Pubmed]
  12. Prevalence of serious eosinophilia and incidence of Churg-Strauss syndrome in a cohort of asthma patients. Loughlin, J.E., Cole, J.A., Rothman, K.J., Johnson, E.S. Ann. Allergy Asthma Immunol. (2002) [Pubmed]
  13. Montelukast reduces peripheral blood eosinophilia but not tissue eosinophilia or symptoms in a patient with eosinophilic gastroenteritis and esophageal stricture. Daikh, B.E., Ryan, C.K., Schwartz, R.H. Ann. Allergy Asthma Immunol. (2003) [Pubmed]
  14. The effect of montelukast on bronchial hyperreactivity in preschool children. Hakim, F., Vilozni, D., Adler, A., Livnat, G., Tal, A., Bentur, L. Chest (2007) [Pubmed]
  15. Montelukast, a leukotriene receptor antagonist, in combination with loratadine, a histamine receptor antagonist, in the treatment of chronic asthma. Reicin, A., White, R., Weinstein, S.F., Finn, A.F., Nguyen, H., Peszek, I., Geissler, L., Seidenberg, B.C. Arch. Intern. Med. (2000) [Pubmed]
  16. Telithromycin, but not montelukast, increases the plasma concentrations and effects of the cytochrome P450 3A4 and 2C8 substrate repaglinide. Kajosaari, L.I., Niemi, M., Backman, J.T., Neuvonen, P.J. Clin. Pharmacol. Ther. (2006) [Pubmed]
  17. Inhibitory effect of a leukotriene receptor antagonist (montelukast) on neurokinin A-induced bronchoconstriction. Crimi, N., Pagano, C., Palermo, F., Mastruzzo, C., Prosperini, G., Pistorio, M.P., Vancheri, C. J. Allergy Clin. Immunol. (2003) [Pubmed]
  18. Montelukast prevents antigen-induced mucociliary dysfunction in sheep. Sabater, J.R., Wanner, A., Abraham, W.M. Am. J. Respir. Crit. Care Med. (2002) [Pubmed]
  19. Effect of the addition of montelukast to inhaled fluticasone propionate on airway inflammation. O'Sullivan, S., Akveld, M., Burke, C.M., Poulter, L.W. Am. J. Respir. Crit. Care Med. (2003) [Pubmed]
  20. The effect of cysteinyl leukotrienes on growth of eosinophil progenitors from peripheral blood and bone marrow of atopic subjects. Braccioni, F., Dorman, S.C., O'byrne, P.M., Inman, M.D., Denburg, J.A., Parameswaran, K., Baatjes, A.J., Foley, R., Gauvreau, G.M. J. Allergy Clin. Immunol. (2002) [Pubmed]
  21. Inflammatory basis of exercise-induced bronchoconstriction. Hallstrand, T.S., Moody, M.W., Wurfel, M.M., Schwartz, L.B., Henderson, W.R., Aitken, M.L. Am. J. Respir. Crit. Care Med. (2005) [Pubmed]
  22. Leukotriene D(4) enhances immunoglobulin production in CD40-activated human B lymphocytes. Lamoureux, J., Stankova, J., Rola-Pleszczynski, M. J. Allergy Clin. Immunol. (2006) [Pubmed]
  23. A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization. Wang, S., Gustafson, E., Pang, L., Qiao, X., Behan, J., Maguire, M., Bayne, M., Laz, T. J. Biol. Chem. (2000) [Pubmed]
  24. Comparison of fluticasone propionate-salmeterol combination therapy and montelukast in patients who are symptomatic on short-acting beta(2)-agonists alone. Calhoun, W.J., Nelson, H.S., Nathan, R.A., Pepsin, P.J., Kalberg, C., Emmett, A., Rickard, K.A., Dorinsky, P. Am. J. Respir. Crit. Care Med. (2001) [Pubmed]
  25. Effect of combined montelukast and desloratadine on the early asthmatic response to inhaled allergen. Davis, B.E., Todd, D.C., Cockcroft, D.W. J. Allergy Clin. Immunol. (2005) [Pubmed]
  26. Combination Therapy with a Long-Acting beta-Agonist and a Leukotriene Antagonist in Moderate Asthma. Deykin, A., Wechsler, M.E., Boushey, H.A., Chinchilli, V.M., Kunselman, S.J., Craig, T.J., Dimango, E., Fahy, J.V., Kraft, M., Leone, F., Lazarus, S.C., Lemanske, R.F., Martin, R.J., Pesola, G.R., Peters, S.P., Sorkness, C.A., Szefler, S.J. Am. J. Respir. Crit. Care Med. (2007) [Pubmed]
  27. Comparative efficacy and anti-inflammatory profile of once-daily therapy with leukotriene antagonist or low-dose inhaled corticosteroid in patients with mild persistent asthma. Dempsey, O.J., Kennedy, G., Lipworth, B.J. J. Allergy Clin. Immunol. (2002) [Pubmed]
  28. Toll-like receptor agonists differentially regulate cysteinyl-leukotriene receptor 1 expression and function in human dendritic cells. Thivierge, M., Stankova, J., Rola-Pleszczynski, M. J. Allergy Clin. Immunol. (2006) [Pubmed]
  29. Hepatic microsomal metabolism of montelukast, a potent leukotriene D4 receptor antagonist, in humans. Chiba, M., Xu, X., Nishime, J.A., Balani, S.K., Lin, J.H. Drug Metab. Dispos. (1997) [Pubmed]
  30. Nasal cytokine modulation by montelukast in allergic children: a pilot study. Ciprandi, G., Frati, F., Marcucci, F., Sensi, L., Tosca, M.A., Milanese, M., Ricca, V. Allergie et immunologie. (2003) [Pubmed]
  31. Montelukast regulates eosinophil protease activity through a leukotriene-independent mechanism. Langlois, A., Ferland, C., Tremblay, G.M., Laviolette, M. J. Allergy Clin. Immunol. (2006) [Pubmed]
  32. A randomized, double-blind trial of the effect of treatment with montelukast on bronchial hyperresponsiveness and serum eosinophilic cationic protein (ECP), soluble interleukin 2 receptor (sIL-2R), IL-4, and soluble intercellular adhesion molecule 1 (sICAM-1) in children with asthma. Stelmach, I., Jerzynska, J., Kuna, P. J. Allergy Clin. Immunol. (2002) [Pubmed]
  33. Response to montelukast among subgroups of children aged 2 to 14 years with asthma. Meyer, K.A., Arduino, J.M., Santanello, N.C., Knorr, B.A., Bisgaard, H. J. Allergy Clin. Immunol. (2003) [Pubmed]
  34. The national montelukast survey. Barnes, N., Thomas, M., Price, D., Tate, H. J. Allergy Clin. Immunol. (2005) [Pubmed]
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