Platelet P2Y12 receptor antagonist pharmacokinetics and pharmacodynamics: A foundation for distinguishing mechanisms of bleeding and anticipated risk for platelet-directed therapies.

Published

Journal Article (Review)

The platelet P2Y12 receptor is involved in all aspects of arterial thrombosis, including adhesion, activation, aggregation, secretion and development of a stable aggregate on which coagulation proteins can assemble and fibrin strands can mesh. Inhibition of the P2Y12 receptor has been shown convincingly to reduce cardiovascular events among patients with acute coronary syndromes (ACS) and in patients undergoing percutaneous intervention (PCI). Current studies are exploring whether there is a threshold of platelet aggregation below which only more bleeding occurs, without a concomitant reduction in clinical events. The following review considers the potential relevance of reversible and irreversible mechanisms of P2Y12 inhibition to bleeding risk, posing the question, "Is it not only how much but how a platelet P2Y12 receptor is inhibited that determines the attributable safety profile?"

Full Text

Duke Authors

Cited Authors

  • Becker, RC; Gurbel, PA

Published Date

  • March 2010

Published In

  • Thromb Haemost

Volume / Issue

  • 103 / 3

Start / End Page

  • 535 - 544

PubMed ID

  • 20135066

Pubmed Central ID

  • 20135066

Electronic International Standard Serial Number (EISSN)

  • 2567-689X

Digital Object Identifier (DOI)

  • 10.1160/TH09-07-0491

Language

  • eng

Conference Location

  • Germany