Leukotrienes (LTs), including cysteinyl LTs (CysLTs) and LTB₄, are potent lipid mediators that have a role in the pathophysiology of asthma. At least two receptor subtypes for CysLTs, CysLT₁ and CysLT₂, have been identified. The activation of the CysLT₁ receptor is responsible for most of the pathophysiological effects of CysLTs in asthma, including increased airway smooth muscle activity, microvascular permeability, and airway mucus secretion. LTB₄ might have a role in severe asthma, asthma exacerbations, and the development of airway hyperresponsiveness. CysLT₁ receptor antagonists can be given orally as monotherapy in patients with mild persistent asthma, but these drugs are generally less effective than inhaled glucocorticoids. Combination of CysLT₁ receptor antagonists and inhaled glucocorticoids in patients with more severe asthma may improve asthma control and enable the dose of inhaled glucocorticoids to be reduced while maintaining similar efficacy. The identification of subgroups of asthmatic patients who respond to CysLT₁ receptor antagonists is relevant for asthma management as the response to these drugs is variable. CysLT₁ receptor antagonists have a potential anti‐remodelling effect that might be important for preventing or reversing airway structural changes in patients with asthma. This review discusses the role of LTs in asthma and the role of LT modifiers in asthma treatment.

Cite this as: P. Montuschi and M. L. Peters‐Golden, Clinical & Experimental Allergy, 2010 (40) 1732–1741.