The pharmacokinetics and pharmacodynamics of prasugrel in healthy Chinese, Japanese, and Korean subjects compared with healthy Caucasian subjects.

Prasugrel is a novel thienopyridine prodrug metabolised to an active metabolite that binds irreversibly to the platelet P2Y12 receptor and inhibits adenosine diphosphate (ADP)-induced platelet aggregation. We compared prasugrel pharmacokinetics, pharmacodynamics, and tolerability in healthy Chinese,...

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Published in:European Journal of Clinical Pharmacology Vol. 66; no. 2; pp. 127 - 136
Main Authors: Small DS, Kothare P, Yuen E, Lachno DR, Li YG, Winters KJ, Farid NA, Ni L, Jakubowski JA, Salazar DE, Thieu VT, Payne CD
Format: clinical trial equations & formulas research tables/charts Journal Article
Published: Springer Nature Feb2010
Online Access:View this record in EBSCOhost
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      dt: Feb2010
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      pub: Springer Nature
      place: New York, New York
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        2010536077
        10.1007/s00228-009-0737-1
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        atl: The pharmacokinetics and pharmacodynamics of prasugrel in healthy Chinese, Japanese, and Korean subjects compared with healthy Caucasian subjects.
      aug:
        au:
          Small DS
          Kothare P
          Yuen E
          Lachno DR
          Li YG
          Winters KJ
          Farid NA
          Ni L
          Jakubowski JA
          Salazar DE
          Thieu VT
          Payne CD
        affil: Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center Indianapolis 46285 USA
      sug:
        subj:
          Platelet Aggregation Inhibitors Pharmacokinetics
          Adult
          Asians
          Body Weight
          Clinical Trials
          Descriptive Statistics
          Female
          Funding Source
          Human
          Male
          Pharmacy and Pharmacology
          Platelet Aggregation Inhibitors Pharmacodynamics
          White Persons
          Adult: 19-44 years
          Female
          Male
      ab: Prasugrel is a novel thienopyridine prodrug metabolised to an active metabolite that binds irreversibly to the platelet P2Y12 receptor and inhibits adenosine diphosphate (ADP)-induced platelet aggregation. We compared prasugrel pharmacokinetics, pharmacodynamics, and tolerability in healthy Chinese, Japanese, Korean and Caucasian subjects. In an open-label, single-centre, parallel-design study, 89 healthy subjects (25 Chinese, 20 Japanese, 22 Korean and 22 Caucasian) aged 20-65 years were given a prasugrel 60-mg loading dose (LD) followed by daily 10-mg maintenance doses (MD) for 7 days and then 5-mg MD for 10 days. Plasma concentrations of prasugrel's active metabolite and inhibition of ADP-induced platelet aggregation (IPA) were determined. Mean exposure to prasugrel's active metabolite in all treatment regimens was higher in each of the Asian groups than in the Caucasian group, although there was considerable overlap between individual exposure estimates in Asians and Caucasians. The mean IPA was also higher in Asians than in Caucasians following a prasugrel 60-mg LD, although the difference did not consistently achieve statistical significance. Prasugrel 10-mg or 5-mg MD produced statistically significantly higher IPA in each Asian group compared with that in the Caucasians. Prasugrel was well tolerated during the LD and MD regimens by all groups. Mean exposure to the prasugrel active metabolite following prasugrel 60-mg LD and during daily 10-mg or 5-mg MD was higher in each of the Asian groups than in the Caucasian group, which resulted in greater platelet inhibition.
      pubtype: Academic Journal
      doctype:
        clinical trial
        equations & formulas
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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