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Inhibition of CysLT-induced bronchial smooth muscle contraction likely is involved in the therapeutic effects of these agents to relieve the symptoms of asthma.

Leukotriene-Synthesis Inhibitors The formation of leukotrienes depends on lipoxygenation of arachidonic acid by 5-lipoxygenase. Zileuton is a potent and selective inhibitor of 5-lipoxygenase activity and thus blocks the formation of all 5-lipoxygenase products. Thus, in addition to inhibiting the formation of the cys-LTs, zileuton also inhibits the formation of leukotriene B4 (LTB4), a potent chemotactic autacoid, and other eicosanoids that depend on leukotriene A4 (LTA4) synthesis. Logically, the therapeutic effects of a 5-lipoxygenase inhibitor would include all those observed with the CysLT-receptor antagonists, as well as other effects that may result from inhibiting the formation of LTB4 and other 5-lipoxygenase products.

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