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[Prasugrel, a new thienopyridine].

K Schrör1, K Huber

  • 1Institutes für Pharmakologie und Klinische Pharmakologie, Universitätsklinikum Düsseldorf, Universitätsstrasse 1, Geb. 22.21, 40225 Düsseldorf. karsten.schroer@uni-duesseldorf.de

Hamostaseologie
|December 7, 2007
PubMed
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Prasugrel, a new antiplatelet drug, shows improved potency and faster action compared to clopidogrel due to better conversion to its active form. This may lead to enhanced clinical efficacy with potentially less variability.

Area of Science:

  • Pharmacology
  • Cardiovascular Medicine
  • Drug Development

Background:

  • Thienopyridines like clopidogrel are oral antiplatelet agents, but exhibit interindividual efficacy variations (clopidogrel resistance).
  • Prasugrel is a novel thienopyridine with similar antiplatelet mechanisms to clopidogrel, targeting the P2Y(12) ADP receptor.

Purpose of the Study:

  • To compare the pharmacological properties of prasugrel and clopidogrel.
  • To investigate the pharmacokinetic differences influencing their antiplatelet activity.

Main Methods:

  • Comparison of prodrug conversion rates to active metabolites.
  • Assessment of oral potency and onset of action.
  • Evaluation of interindividual variability in antiplatelet efficacy.

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Main Results:

  • Prasugrel demonstrates higher conversion to its active metabolite (R-138727) compared to clopidogrel (10-15%).
  • Prasugrel exhibits greater oral potency and a more rapid onset of action than clopidogrel.
  • Improved pharmacokinetics of prasugrel suggest reduced interindividual variability and potentially less 'resistance'.

Conclusions:

  • Prasugrel's enhanced conversion and pharmacokinetic profile may offer improved antiplatelet efficacy over clopidogrel.
  • Further clinical trials are needed to confirm efficacy and assess bleeding risk in patients undergoing percutaneous coronary intervention (PCI).