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Mini-Review TheScientificWorldJOURNAL (2010) 10, 2403–2413 ISSN 1537-744X; DOI 10.1100/tsw.2010.229 Montelukast: More than a Cysteinyl Leukotriene Receptor Antagonist? 1, 2 3 Gregory R. Tintinger *, Charles Feldman , Annette J. Theron , and Ronald Anderson3 1 Department of Internal Medicine, Faculty of Health Sciences, University of Pretoria, 2 South Africa; Department of Internal Medicine, Faculty of Health Sciences, 3 University of the Witwatersrand, Johannesburg, South Africa; Medical 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 E-mail: grtintinger@; feldmanc@medicine.wits.ac.za; atheron@postillion.up.ac.za; ronald.anderson@up.ac.za Received August 6, 2010; Revised November 11, 2010, Accepted November 15, 2010; Published December 14, 2010 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