Montelukast is a selective leukotriene receptor antagonist that has been sh
own to be effective in the treatment of chronic asthma. It is approved in m
ore than 70 countries for patients 6 years of age and older. For adults (gr
eater than or equal to 15 years of age), a 10-mg film-coated tablet (FCT) i
s available, and for children (aged 6 to 14 years), a 5-mg chewable tablet
(CT) is available. The adult montelukast dose (10-mg FCT) was selected on t
he basis of classic dose-ranging studies as the lowest dose that produces m
aximal improvement in both measures of airway function and patient-reported
outcomes in chronic asthma and in the attenuation of exercise-induced bron
choconstriction. The strategy used for the pediatric dose selection for mon
telukast was based on the determination of a CT dose that would provide an
overall systemic exposure to montelukast in children similar to that in adu
lts who receive a IO-mg FCT dose. Because montelukast was to be given chron
ically for the treatment of asthma, the area under the plasma concentration
-time curve was considered to be the pharmacokinetic measurement that best
represented systemic exposure to the drug. A 5-mg CT yielded a comparable s
ingle-dose area under the plasma concentration-time curve profile to that o
f the adult 10-mg FCT dose and, therefore, was selected as the pediatric do
se for children aged 6 to 14 years with asthma. Subsequently, 2 studies of
efficacy and tolerability validated the choice of the 5-mg CT dose.