title: Montelukast: more than a cysteinyl leukotriene receptor antagonist?
abstract: The prototype cysteinyl leukotriene receptor antagonist, montelukast, is generally considered to have a niche application in the therapy of exercise- and aspirin-induced asthma. It is also used as add-on therapy in patients whose asthma is poorly controlled with inhaled corticosteroid monotherapy, or with the combination of a long-acting beta(2)-agonist and an inhaled corticosteroid. Recently, however, montelukast has been reported to possess secondary anti-inflammatory properties, apparently unrelated to conventional antagonism of cysteinyl leukotriene receptors. These novel activities enable montelukast to target eosinophils, monocytes, and, in particular, the corticosteroid-insensitive neutrophil, suggesting that this agent may have a broader spectrum of anti-inflammatory activities than originally thought. If so, montelukast is potentially useful in the chemotherapy of intermittent asthma, chronic obstructive pulmonary disease, cystic fibrosis, and viral bronchiolitis, which, to a large extent, involve airway epithelial cell/neutrophil interactions. The primary objective of this mini-review is to present evidence for the cysteinyl leukotriene-independent mechanisms of action of montelukast and their potential clinical relevance.
authors.affiliation: Department of Internal Medicine, Faculty of Health Sciences, University of Pretoria, South Africa. grtintinger@gmail.com
authors.forename: Gregory R
authors.initials: GR
authors.lastname: Tintinger
authors.forename: Charles
authors.initials: C
authors.lastname: Feldman
authors.forename: Annette J
authors.initials: AJ
authors.lastname: Theron
authors.forename: Ronald
authors.initials: R
authors.lastname: Anderson
mesh_terms: D000085:Acetates / Q000494:pharmacology / Q000627:therapeutic use*; D018927:Anti-Asthmatic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D000893:Anti-Inflammatory Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001249:Asthma / Q000188:drug therapy; D003521:Cyclopropanes; D006801:Humans; D020024:Leukotriene Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy; D011804:Quinolines / Q000494:pharmacology / Q000627:therapeutic use*; D018077:Receptors, Leukotriene / Q000378:metabolism; D013440:Sulfides
chemical_list: D000085:Acetates; D018927:Anti-Asthmatic Agents; D000893:Anti-Inflammatory Agents; D003521:Cyclopropanes; D020024:Leukotriene Antagonists; D011804:Quinolines; D018077:Receptors, Leukotriene; D013440:Sulfides; C083169:leukotriene D4 receptor; C093875:montelukast