In the past decade, heightened emphasis has been placed on the importance of inflammation in the pathogenesis of asthma. Although corticosteroids have remained the primary anti-inflammatory agents in the management of the persistent asthmatic, new classes of drugs have recently been added. The leukotriene receptor antagonists (LTRAs) are the first new approach in asthma therapy in the past 25 years and the first class of drugs to target specific components of the inflammatory process. These drugs reverse the primary biological effects of the cysteinyl leukotrienes in relation to the pathogenesis of asthma including bronchoconstriction, mucus hypersecretion, and airway inflammation. The LTRAs have demonstrated efficacy against exercise- and allergen-induced bronchoconstriction, aspirin-sensitive asthma, and additive benefit in symptomatic moderate asthmatics on maintenance inhaled corticosteroids, as well as potential steroid-sparing effects. Finally, although evidence for their role as first-line controller agents for the management of mild persistent asthma has grown stronger in recent years, this role continues to evolve.