A leukotriene antagonist (sometimes referred to as a leukast) is a drug that inhibits leukotrienes, which are fatty compounds produced by the immune system that cause inflammation in asthma and bronchitis, and constrict airways.
Leukotriene inhibitors (or modifiers), such as montelukast (trade names Singulair and Montelo-10), zafirlukast, pranlukast and zileuton, are used to treat those diseases. They are less effective than corticosteroids and are thus less preferred in the treatment of 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.
Antagonism of cysteinyl-leukotriene type 1 receptors
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.
- Fanta CH (March 2009). "Asthma". N Engl J Med 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689.
- Jawien, J.; Gajda, M.; Rudling, M.; Mateuszuk, L.; Olszanecki, R.; Guzik, T. J.; Cichocki, T.; Chlopicki, S.; Korbut, R. (March 2006). "Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice". European Journal of Clinical Investigation 36 (3): 141–146. doi:10.1111/j.1365-2362.2006.01606.x. PMID 16506957.
|This biochemistry article is a stub. You can help Wikipedia by expanding it.|