Platelet inhibitory activity and pharmacokinetics of prasugrel (CS-747) a novel thienopyridine P2Y 12 inhibitor: A multiple-dose study in healthy humans†.

Autor: Matsushima, Nobuko, Jakubowski, Joseph A., Asai, Fumitoshi, Naganuma, Hideo, Brandt, John T., Hirota, Takashi, Freestone, Stephen, Winters, Kenneth J.
Předmět:
Zdroj: Platelets; Jun2006, Vol. 17 Issue 4, p218-226, 8p
Abstrakt: This double-blind, placebo-controlled trial evaluated the safety, pharmacodynamics, and pharmacokinetics of prasugrel (CS-747, LY640315), a novel thienopyridine P2Y 12 ADP receptor antagonist, during multiple oral dosing in healthy subjects. Eighteen subjects received placebo, or prasugrel 2.5 or 10  mg, orally, daily for 10 days. Adverse events were recorded and blood samples for measurement of platelet aggregation, bleeding time, and prasugrel metabolite concentrations were obtained. Two bleeding events were experienced in the prasugrel 10  mg dose group and one in the placebo group. Neither of the events was considered serious. ADP-induced platelet aggregation accumulated over the 10-day study period, reaching a steady state by days 2–4 following administration of prasugrel 10  mg daily. Limited inhibition of platelet aggregation was obtained with prasugrel 2.5  mg. In the 10-mg dose group at day 5, 4  h postdose, with 20  µM ADP as the agonist, inhibition of platelet aggregation was 61.2  ±  5.6 vs. 17.9  ±  6.2% in the placebo group ( P    [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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