This article summarizes data from several trials in order to provide clinical investigators with an understanding of the pharmacokinetics of enzalutamide. Collectively, the results show that enzalutamide has a half-life of 5.8 days, achieves steady state by day 28, accumulates 8.3-fold with once-daily dosing, shows approximate dose proportionality from 30–360 mg/day, and has ≤30 % intersubject variability.

In addition, enzalutamide is primarily eliminated by hepatic metabolism, while renal excretion is an insignificant elimination pathway for enzalutamide and its active metabolite, N-desmethyl enzalutamide. Exposure to enzalutamide active moieties is not affected by food or baseline mild or moderate hepatic impairment.

In an exposure-response analysis of overall survival in patients with mCRPC, active treatment C trough quartile groups for a fixed dose of 160 mg/day were uniformly beneficial relative to placebo, and there was no specific threshold of plasma concentrations in patients receiving enzalutamide that was associated with achieving a statistically significant better response; therefore, similar efficacy was observed in patients across the concentration/exposure range associated with a fixed oral dose of enzalutamide 160 mg/day.