Alectinib, an anaplastic lymphoma kinase (ALK) inhibitor, is approved for 
treatment of patients with ALK+ non-small cell lung cancer who have progressed, 
on or are intolerant to, crizotinib. This study assessed the effect of a 
high-fat meal and the proton pump inhibitor, esomeprazole, on the 
pharmacokinetics (PK) of alectinib. This was an open-label, 2-group study in 
healthy subjects. In group 1 (n = 18), subjects were randomly assigned to a 
2-treatment (A, fasted conditions; B, following a high-fat meal), 2-sequence (AB 
or BA) crossover assessment, separated by a 10-day washout. In group 2 (n = 24), 
subjects were enrolled in a 2-period, fixed-sequence crossover assessment to 
evaluate the effect of esomeprazole. PK parameters were evaluated for alectinib, 
its major similarly active metabolite, M4, and the combined exposure of 
alectinib and M4. Administration of alectinib following a high-fat meal 
substantially increased the combined exposure of alectinib and M4 to 331% 
(90%CI, 279%-393%) and 311% (90%CI, 273%-355%) for Cmax and AUC0-∞ , 
respectively, versus fasted conditions. Coadministration of esomeprazole had no 
clinically relevant effect on the combined exposure of alectinib and M4. 
Alectinib should be administered under fed conditions to maximize its 
bioavailability, whereas no restrictions are required with antisecretory agents.