The clinical pharmacology of brigatinib, an orally administered anaplastic lymphoma kinase (ALK) inhibitor, approved for the treatment of metastatic ALK-positive non-small cell lung cancer has been extensively characterized based on data from phase I–III clinical trials, as well as integrated population pharmacokinetic, physiologically based pharmacokinetic, and exposure–response analyses.

Sex, age, race, body weight, food, and mild or moderate renal or hepatic impairment do not have a clinically meaningful effect on the pharmacokinetics of brigatinib.

Exposure–response analyses confirm the favorable benefit versus risk profile of the approved titration dosing regimen of a 7-day lead-in at 90 mg once daily followed by 180 mg once daily.