The demonstration that leukotrienes, mainly cysteinyl leukotrienes, have biological properties relevant to the pathogenesis of asthma has stimulated the development of many therapeutic compounds to block these deleterious effects. Two main classes of leukotriene modulators have been developed: CysLT1 receptor antagonists and leukotriene synthesis inhibitors. This article reviews the pharmacodynamics, the effects on baseline airway function, the protective effects in airway challenges as well as the results in chronic asthma of the different leukotriene modulators. In addition, the complementary anti-inflammatory effect of leukotriene modulators to that of corticosteroids and H1-histamine receptor antagonists is reviewed. Finally, a concise overview of the clinical responsiveness to this new class of drug, the safety and the drug interactions as well as the place in the strategies of treatment for asthmatic patients of the leukotriene modulators is also provided.