The cysteinyl leukotrienes (LTs) are chemical mediators that are thought to contribute to the pathophysiologic condition of asthma and other inflammatory diseases. The biological effects of the cysteinyl LTs in the lung are pleiotropic, including both bronchoconstrictor and a growing list of nonbronchoconstrictor activities that extend to inflammatory cell recruitment, vascular leakage, mucus production, neuronal dysfunction, and airways remodeling. This spectrum of effects of cysteinyl LTs is consistent with an expanded view of asthma that extends beyond simply bronchoconstriction and inflammation. Consequently, the clinical efficacy of cysteinyl LT receptor antagonists (LTRAs) in asthma may be related to antagonism of more than cysteinyl LT-induced bronchoconstriction. The relationship of antagonism of the multiple effects of cysteinyl LTs by cysteinyl LTRAs to their utility in the therapy of asthma is addressed, and the preclinical and clinical pharmacology of cysteinyl LTRAs is reviewed.