Leukotriene inhibitors

Antileukotrienes
Drug class
Class identifiers
Mechanism of action	• Enzyme inhibition  • Receptor antagonism
Biological target	• Enzymes: 5-LOX; FLAP  • Receptors: CysLTRs

An antileukotriene is a drug which functions as a leukotriene-related enzyme inhibitor (arachidonate 5-lipoxygenase) or leukotriene receptor antagonist (cysteinyl leukotriene receptors) and consequently opposes the function of these inflammatory mediators; leukotrienes are produced by the immune system and serve to promote bronchoconstriction, inflammation, microvascular permeability, and mucus secretion in asthma and COPD. Leukotriene receptor antagonists are sometimes colloquially referred to as leukasts.

Leukotriene receptor antagonists, such as montelukast, zafirlukast, and pranlukast, and 5-lipoxygenase inhibitors, like zileuton and hypericum perforatum, can be used to treat these diseases. They are less effective than corticosteroids for treating asthma, but more effective for treating certain mast cell disorders.

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

Drugs that inhibit the 5-lipoxygenase enzyme will inhibit the synthetic pathway of leukotriene metabolism; drugs such as MK-886 that block the 5-lipoxygenase activating protein (FLAP) inhibit functioning of the 5-lipoxygenase enzyme and may help in treating atherosclerosis.

Examples of 5-LOX inhibitors include drugs, such as meclofenamate sodium and zileuton.

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