Clinical Pharmacokinetic Studies of Enzalutamide

Enzalutamide
DOI: 10.1007/s40262-015-0271-5 Publication Date: 2015-04-27T08:38:48Z
ABSTRACT
Oral enzalutamide (160 mg once daily) is approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC). This article describes pharmacokinetics and its active metabolite N-desmethyl enzalutamide. Results are reported from five clinical studies. In a dose-escalation study (n = 140), half-life was 5.8 days, steady state achieved by day 28, accumulation 8.3-fold, exposure approximately dose proportional 30–360 mg/day, intersubject variability ≤30 %. mass balance 6), primarily eliminated hepatic metabolism. Renal excretion an insignificant elimination pathway food-effect 60), food did not have meaningful effect on area under plasma concentration–time curve (AUC) or enzalutamide, in impairment study, AUC sum plus similar men with mild 6) moderate 8) (Child–Pugh Class A B) versus normal function 14). phase III trial, exposure-response analysis steady-state predose (trough) concentrations (C trough) overall survival 1103) showed that C trough quartiles 160 mg/day were uniformly beneficial relative to placebo, no threshold associated statistically significant better response. Enzalutamide has predictable pharmacokinetics, low variability. Similar efficacy observed patients across concentration/exposure range fixed oral mg/day.
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