The cysteinyl leukotrienes are potent mediators of airway narrowing derived from the lipoxygenation of arachidonic acid and the adduction of glutathione to this eicosanoid backbone. In lower animals and humans, the cysteinyl leukotrienes are among the most potent airway contractile substances ever identified. Furthermore, these moieties can be recovered from the urine during induced or spontaneous asthma attacks. Most important, inhibition of the synthesis of the leukotrienes or prevention of their action at the CysLT1 receptor is associated with an improvement in the airway dysfunction that occurs in both induced and spontaneous asthma. These data indicate that the cysteinyl leukotrienes have a clinically significant role in the airway obstruction that characterizes asthma.