Premium
Effects of Food on the Pharmacokinetics of Edoxaban, an Oral Direct Factor Xa Inhibitor, in Healthy Volunteers
Author(s) -
Mendell Jeanne,
Tachibana Masaya,
Shi Minggao,
Kunitada Satoshi
Publication year - 2011
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270010370974
Subject(s) - pharmacokinetics , edoxaban , medicine , pharmacology , rivaroxaban , warfarin , atrial fibrillation
The primary objective of this study was to assess the effect of a standard high‐fat meal on the single‐dose (60 mg) pharmacokinetics (PK) of edoxaban in healthy Japanese and Caucasian male volunteers matched by body mass index. This was an open‐label, randomized, 2‐period crossover study. All 32 enrolled volunteers completed the study per protocol. Both serial blood and urine samples were collected, and edoxaban concentrations were analyzed by a validated liquid chromatography/tandem mass spectrometry method. Activated partial thromboplastin and prothrombin times were obtained as measures of pharmacodynamic effect. The point estimates of the geometric mean ratios (fed/fasted) for AUC 0‐t , AUC 0‐∞ , and C max demonstrated modest increases ranging from 6% to 22% across PK parameters for both race cohorts. The disposition was similar in both Japanese and Caucasian matched volunteers with slightly higher AUC values (ranging from 7%‐9%) in Caucasians. There were no serious adverse events during the study. All drug‐related adverse events were mild and self‐limited, and none were bleeding related. Both Japanese and Caucasian volunteers demonstrated a modest but clinically insignificant food effect. It was concluded that edoxaban can be administered without regard to food.