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The Absence of a Clinically Significant Effect of Food on the Single Dose Pharmacokinetics of Vorapaxar, a PAR-1 Antagonist, in Healthy Adult Subjects
Ist Teil von
Clinical pharmacology in drug development, 2013-10, Vol.2 (4), p.310-315
Ort / Verlag
United States: Blackwell Publishing Ltd
Erscheinungsjahr
2013
Link zum Volltext
Quelle
Wiley-Blackwell subscription journals
Beschreibungen/Notizen
In this open‐label, randomized, 2‐period crossover study, 16 healthy subjects received a single oral 2.5‐mg dose of vorapaxar in the fed (i.e., standardized high‐fat breakfast) and fasted (i.e., an overnight fast) state with a 6‐week washout. Plasma samples for vorapaxar assay were obtained pre‐dose and up to 72 hours post‐dose. Least squares (LS) geometric mean AUC0–72 hr and Cmax were analyzed by ANOVA. If 90% confidence intervals (CI) for the geometric mean ratios (GMRs; fed/fasted) of AUC0–72 hr and Cmax were within the 50–200% range, then food was deemed not to have a clinically important effect. The LS geometric mean (90% CI) AUC0–72 hr and Cmax of vorapaxar in the fasted state were 314 (284–348) ng hr/mL and 23.4 (20.7–26.4) ng/mL, respectively. The GMRs (fed/fasted) and 90% CIs for AUC0–72 hr and Cmax were 96.9 (92.2–102) and 79.1 (67.6–92.5), respectively. Vorapaxar was generally safe and well tolerated in the presence and absence of food. Concomitant food decreased the rate (i.e., 21% reduction in Cmax and 45‐min delay in Tmax) with no effect on the extent of vorapaxar absorption when administered as a single 2.5‐mg dose. Thus, vorapaxar can be administered without regard to food.