Use of indacaterol for the treatment of COPD: a pharmacokinetic evaluation

Indacaterol is a β2-agonist with a rapid onset of action and a bronchodilating effect that lasts for 24 h.

This review considers indacaterol in chronic obstructive pulmonary disease patients, in whom it is rapidly absorbed into the systemic circulation with serum levels measurable after 5 min and Cmax being reached approximately 15 min post-dose. Its disposition kinetics are characterized by at least two phases, a relatively fast decline of the concentrations within the first 12 h, followed by a terminal elimination phase. The increase in systemic exposure is dose-proportional, but systemic concentrations are low at the recommended doses. Indacaterol is relatively highly bound to plasma proteins regardless of concentration. Metabolic clearance and/or biliary clearance account for the majority of its systemic excretion. Weight, age, gender and ethnicity significantly influence its pharmacokinetic profile, but it is not necessary to adjust the dose based on these covariates. Substrates, inhibitors or inducers of UGT1A1 and CYP3A may also affect the pharmacokinetic profile of indacaterol.

Blood concentrations of indacaterol are unable to predict its bronchodilator effects. Furthermore, at the recommended doses, systemic concentrations of indacaterol are low and this is the likely reason for its safe profile.