Leukotrienes, and especially cysteinyl leukotrienes have been shown to be involved in many processes that play a role in asthma pathophysiology: eosinophil recruitment, the most characteristic processes of asthma pathogenesis, increased mucosal secretion, which impairs the normal process of airway clearance and favors the development of mucus plugs, mucosal edema, caused by increased vascular permeability and bronchoconstriction, leading to smooth muscle hypertrophy. Latest progress in the understanding of chronic asthma pathology events underline the leukotriene synthesis pathway enzymes and different leukotriene receptors as potential targets of asthma treatment in children. Agents inhibiting the production of leukotrienes or agents antagonising their receptor's action, attract attention. Studies on molecular mechanisms of leukotrienes action have led to the development and patents of potential drugs including new 5-lipoxygenase inhibitors, 5-lipoxygenase-activating protein (FLAP) inhibitors, leukotriene B4 receptor antagonists, or nanoparticulate leukotriene receptor antagonist formulations.