Strategies for inhibition of cysteinyl leukotriene effects include antagonism of
cysteinyl leukotriene receptors and inhibition of 5-lipoxygenase activity. In experimental
challenge studies in asthmatic patients, these compounds can inhibit bronchoconstriction
in response to exercise, aspirin and allergen. Results from clinical
studies using receptor antagonists, such as ICI 204,219 and MK-571, and synthesis
inhibitors, such as zileuton, demonstrate beneficial effects, with improvement in
symptoms and forced expiratory volume in one second (FEV1), and a reduction in
the use of b2-adrenergic relief medication. Further studies are needed to clarify the
exact mechanisms by which these compounds provide beneficial effects.
Strategies for inhibition of cysteinyl leukotriene effects include antagonism of
cysteinyl leukotriene receptors and inhibition of 5-lipoxygenase activity. In experimental
challenge studies in asthmatic patients, these compounds can inhibit bronchoconstriction
in response to exercise, aspirin and allergen. Results from clinical
studies using receptor antagonists, such as ICI 204,219 and MK-571, and synthesis
inhibitors, such as zileuton, demonstrate beneficial effects, with improvement in
symptoms and forced expiratory volume in one second (FEV1), and a reduction in
the use of b2-adrenergic relief medication. Further studies are needed to clarify the
exact mechanisms by which these compounds provide beneficial effects.
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