Montelukast Dose Selection in 6‐ to 14‐Year‐Olds: Comparison of Single‐Dose Pharmacokinetics in Children and Adults

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Abstract
Montelukast, an oral leukotriene‐receptor antagonist, has demonstrated efficacy and tolerability for the treatment of chronic asthma in adults. A once‐daily 10 mg dose (film‐coated tablet) was selected as the optimal adult dose based on dose‐ranging studies. Asthma is a similar disease and is treated with the same medications in children and adults. These observations suggested that a dose of montelukast in children providing overall drug exposure (i.e., montelukast plasma concentrations) similar to that of the 10 mg film‐coated tablet dose in adults would be efficacious, well tolerated, and obviate the need for separate dose‐ranging studies in children. Therefore, the dose of montelukast for 6‐ to 14‐ year‐old children was selected by identifying the chewable tablet dose of montelukast yielding a single‐dose area under the plasma concentration‐time curve (AUC) comparable to that achieved with the adult 10 mg film‐coated tablet dose. Based on this approach, which included dose normalization of data from several pediatric pharmacokinetic studies, a 5 mg chewable tablet dose of montelukast was selected for use in clinical efficacy studies in 6‐ to 14‐year‐old children with asthma.