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Behm MO, Kosoglou T, Miltenburg AM, et al. The Absence of a Clinically Significant Effect of Food on the Single Dose Pharmacokinetics of Vorapaxar, a PAR-1 Antagonist, in Healthy Adult Subjects. Clin Pharmacol Drug Dev. 2013;2(4):310-5doi: 10.1002/cpdd.38.
Behm, M. O., Kosoglou, T., Miltenburg, A. M., Li, J., Statkevich, P., Johnson-Levonas, A. O., Martinho, M., & Fackler, P. (2013). The Absence of a Clinically Significant Effect of Food on the Single Dose Pharmacokinetics of Vorapaxar, a PAR-1 Antagonist, in Healthy Adult Subjects. Clinical pharmacology in drug development, 2(4), 310-5. https://doi.org/10.1002/cpdd.38
Behm, Martin O, et al. "The Absence of a Clinically Significant Effect of Food on the Single Dose Pharmacokinetics of Vorapaxar, a PAR-1 Antagonist, in Healthy Adult Subjects." Clinical pharmacology in drug development vol. 2,4 (2013): 310-5. doi: https://doi.org/10.1002/cpdd.38
Behm MO, Kosoglou T, Miltenburg AM, Li J, Statkevich P, Johnson-Levonas AO, Martinho M, Fackler P. The Absence of a Clinically Significant Effect of Food on the Single Dose Pharmacokinetics of Vorapaxar, a PAR-1 Antagonist, in Healthy Adult Subjects. Clin Pharmacol Drug Dev. 2013 Oct;2(4):310-5. doi: 10.1002/cpdd.38. PMID: 27121935.
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Clin Pharmacol Drug Dev. 2013 Oct;2(4):310-5. doi: 10.1002/cpdd.38.

The Absence of a Clinically Significant Effect of Food on the Single Dose Pharmacokinetics of Vorapaxar, a PAR-1 Antagonist, in Healthy Adult Subjects.

Clinical pharmacology in drug development

Martin O Behm, Teddy Kosoglou, André M M Miltenburg, Jing Li, Paul Statkevich, Amy O Johnson-Levonas, Monika Martinho, Paul Fackler

Affiliations

  1. Merck & Co., Inc., Whitehouse Station, NJ, USA.

PMID: 27121935 DOI: 10.1002/cpdd.38

Abstract

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.

© 2013, The American College of Clinical Pharmacology.

Keywords: PAR-1; food; interaction; pharmacokinetics; vorapaxar

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