Leukotriene antagonist

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


A leukotriene antagonist is a hormone antagonist acting upon leukotrienes.

It has been demonstrated that leukotrienes are implicated in the inflammatory cascade leading to asthma. Leukotriene modifiers are an important therapeutic advance in managing asthma.


There are two main approaches to block the actions of leukotrienes.

Inhibition of the 5-lipoxygenase pathway

Drugs such as zileuton block 5-lipoxygenase, inhibiting the synthetic pathway of leukotriene metabolism, whereas drugs such as MK-886 block the 5-lipoxygenase activating protein (FLAP) and may help in treating atherosclerosis.[1]

Antagonism of cysteinyl-leukotriene type 1 receptors

Agents such as montelukast and zafirlukast block the actions of cysteinyl leukotrienes at the CysLT1 receptor on target cells such as bronchial smooth muscle.

These modifiers have been shown to improve asthma symptoms, reduce asthma exacerbations and limit markers of inflammation such as eosinophil counts in the peripheral blood and bronchoalveolar lavage fluid. This demonstrates that they have anti-inflammatory properties.


  1. Jawien J, Gajda M, Rudling M; et al. (2006). "Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice". Eur. J. Clin. Invest. 36 (3): 141–6. doi:10.1111/j..2006.01606.x.

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