The Centers for Disease Control and Prevention reports that more than 4 million children have been diagnosed with asthma. Currently, there is no treatment that could prevent the development of asthma or change its natural course over long-term follow-up. However, the disease can be controlled using treatments used in clinical practice. For persistent asthma in children aged 5 years and younger, low doses of inhaled glucocorticosteroids are recommended, as well as the administration of montelukast, a leukotriene receptor antagonist. In addition, montelukast is prescribed to patients with allergic rhinitis as an alternative to or in combination with oral antihistamines or nasal corticosteroids. Leukotrienes are lipid mediators that play a key role in acute and chronic inflammation and allergic diseases. They exhibit their biological effects by binding to specific G-protein-coupled receptors. Each subtype of the leukotriene receptor has unique functions and expression patterns. Leukotrienes play an important role in various allergic diseases, including bronchial asthma and allergic rhinitis. Montelukast is a cysteinyl leukotriene receptor-1 antagonist widely used to suppress the inflammatory response in asthma and allergic rhinitis. This review briefly summarizes the biology of leukotrienes and their receptors, recent developments in the field of antileukotriene drugs and the prospects for their different therapeutic applications. The role of antileukotriene drugs and key indications for the use of montelukast in the complex therapy of asthma and allergic rhinitis in children have been determined.