8.5.3 Anti-Leukotrienes as Anti-Inflammatory
Agents for AsthmaLike the other eicosanoids, the leukotrienes are also involved in inflammatory diseases.
Accordingly, leukotriene pathway inhibitors are emerging as important agents. Two
fundamental approaches to the design of leukotriene pathway inhibitors have been
pursued:
- Inhibitors of 5-lipoxygenase (to prevent leukotriene biosynthesis)
- Leukotriene receptor antagonists (to prevent leukotriene binding)
Zileuton (8.81) is an inhibitor of 5-lipoxygenase; montelukast (8.82) and zafirlukast
(8.83) are inhibitors of the leukotriene LTD 4 receptor. All of these agents have demon-
strated efficacy in the treatment of asthma, a common chronic inflammatory disease of
the airways.
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