Cysteinyl leukotrienes are important mediators of asthmatic responses. They are the most potent bronchoconstrictors known; their release is triggered by exposure to inhaled allergens after exercise and after aspirin ingestion by subjects with aspirin-sensitive asthma. The cysteinyl leukotrienes promote inflammatory cell migration into the airways, as well as bone marrow eosinophilopoiesis after allergen inhalation. Leukotriene inhibitors are effective at attenuating asthmatic responses to all of these stimuli and are also effective at treating persistent asthma. These drugs are a viable alternative to low-dose inhaled corticosteroid (ICS) treatment but should be reserved for patients who cannot or will not use ICSs, often because of concerns about potential side effects of ICS treatment, which limits their use, particularly in children. Leukotriene receptor antagonists are also alternatives to long-acting inhaled beta(2)-agonists as add-on therapy to ICSs, but their efficacy together with ICSs is less than that of ICS/long-acting inhaled beta(2)-agonist combinations. Leukotriene receptor antagonists have an excellent safety profile.