4.3 Article

Pharmacodynamics and pharmacokinetics of the novel PAR-1 antagonist vorapaxar (formerly SCH 530348) in healthy subjects

期刊

EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
卷 68, 期 3, 页码 249-258

出版社

SPRINGER HEIDELBERG
DOI: 10.1007/s00228-011-1120-6

关键词

Vorapaxar; SCH 530348; PAR-1 antagonist; Pharmacokinetics; Pharmacodynamics; Platelet aggregation; Thrombin receptor antagonist

资金

  1. Merck, Whitehouse Station, NJ, USA
  2. Merck

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Purpose The aim of our study was to evaluate the pharmacology of vorapaxar (SCH 530348), an oral PAR-1 antagonist, in healthy volunteers. Methods and results In two randomized, placebo-controlled studies, subjects received either single ascending doses of vorapaxar (0.25, 1, 5, 10, 20, or 40 mg; n = 50), multiple ascending doses of vorapaxar (1, 3, or 5 mg/day for 28 days; n = 36), a loading dose (10 or 20 mg) followed by daily maintenance doses (1 mg) for 6 days (n = 12), or placebo. Single 20- and 40-mg doses of vorapaxar completely inhibited thrombin receptor activating peptide (TRAP)-induced platelet aggregation (>80% inhibition) at 1 h and sustained this level of inhibition for >= 72 h. Multiple doses yielded complete inhibition on Day 1 (5 mg/day) and Day 7 (1 and 3 mg/day). Adverse events were generally mild, transient, and unrelated to dose. Conclusion Vorapaxar provided rapid and sustained dose-related inhibition of platelet aggregation without affecting bleeding or clotting times.

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