There was no readily apparent effect of food on the total systemic exposure of alisertib (MLN8237) following single-dose administration of a 50 mg enteric-coated tablet (ECT) formulation. The geometric mean ratio of the area under the curve from time zero to infinity (AUCinf) (fed vs. fasted) was 0.94 (90 % confidence interval 0.68–1.32).

A small (16 %) decrease in the geometric mean maximum observed plasma concentration (C max) was observed when alisertib was administered following a high-fat meal compared with under fasted conditions, and the median time to reach C max (t max) was delayed from 3 to 6 h.

Administration of alisertib ECT in the postprandial state is associated with a reduction in the rate of oral absorption without an effect on the extent of oral absorption. The results of this study support a recommendation that alisertib ECT may be administered without regard for food in future clinical studies unless otherwise specified in the protocols.