Bioequivalence and Pharmacokinetic Study of 2 Edoxaban Tablets in Healthy Chinese Subjects.

The aim was to investigate the bioequivalence of 2 orally administered edoxaban 60-mg tablets and the food effects on the pharmacokinetics of edoxaban. Sixty-four healthy Chinese subjects participated in this open-label, randomized, 2-sequence, 4-period, crossover study. All subjects randomly received 60-mg generic (test) or branded (reference) edoxaban tablet in each period. Plasma edoxaban concentrations were determined using liquid chromatography-tandem mass spectrometry. The pharmacokinetic parameters maximum concentration (C _max ) and area under the concentration-time curve (AUC) were compared to assess bioequivalence. The geometric least-squares mean ratios for C _max , AUC from time 0 to the last measurable time point (AUC _0-t ), and AUC from time 0 extrapolated to infinity (AUC _0-∞ ) were 97.0%, 95.4%, and 96.1%, respectively, in the fasting test, and 98.6%, 100.0%, and 99.8%, respectively, in the fed test. Food increased exposure and prolonged the time to maximum concentration of edoxaban. Both formulations displayed comparable safety profiles, with no serious adverse events reported. The 2 products of edoxaban tablets are bioequivalent and safe in healthy Chinese volunteers. Food may have a modest effect on the pharmacokinetic properties of edoxaban.
(© 2022, The American College of Clinical Pharmacology.)