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Volume 10, Pages 2403-2413
Mini-Review Article

Montelukast: More than a Cysteinyl Leukotriene Receptor Antagonist?

1Department of Internal Medicine, Faculty of Health Sciences, University of Pretoria, South Africa
2Department of Internal Medicine, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, South Africa
3Medical Research Council Unit for Inflammation and Immunity, Department of Immunology, University of Pretoria, and Tshwane Academic Division of the National Health Laboratory Service, Pretoria, South Africa

Received 6 August 2010; Revised 11 November 2010; Accepted 15 November 2010

Academic Editor: Charles N. Serhan

Copyright © 2010 Gregory R. Tintinger et al.


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 β(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 leukotrien–independent mechanisms of action of montelukast and their potential clinical relevance.