Antiplatelet therapy prasugrel: a novel platelet ADP P2Y12 receptor antagonist

Clin Appl Thromb Hemost. 2010 Apr;16(2):170-6. doi: 10.1177/1076029609355589.

Abstract

Novel adenosine diphosphate (ADP) P2Y(12) antagonists, including prasugrel, ticagrelor, cangrelor and elinogrel, are in various phases of clinical development. These ADP P2Y(12) antagonists have advantages over clopidogrel ranging from faster onset to greater and less variable inhibition of platelet function. Novel ADP P2Y(12) antagonists are under investigation to determine whether their use can result in improved antiplatelet activity, faster onset of action, and/or greater antithrombotic effects than clopidogrel, without an unacceptable increase in hemorrhagic or other side effects. Prasugrel (CS-747; LY-640315), a novel third-generation oral thienopyridine, is a specific, irreversible antagonist of the platelet ADP P2Y(12) receptor. Preclinical and early phase clinical studies have shown prasugrel to be characterized by more potent antiplatelet effects, lower interindividual variability in platelet response, and faster onset of activity compared to clopidogrel. Recent findings from large-scale phase III testing showed prasugrel to be more efficacious in preventing ischemic events in patients with acute coronary syndrome (ACS) undergoing percutaneous coronary intervention (PCI); however, this is achieved at the expense of an increased risk of bleeding. Prasugrel provides more rapid and consistent platelet inhibition than clopidogrel.

Publication types

  • Review

MeSH terms

  • Acute Coronary Syndrome / drug therapy
  • Acute Coronary Syndrome / therapy
  • Angioplasty, Balloon, Coronary
  • Aspirin / therapeutic use
  • Clinical Trials, Phase III as Topic
  • Clopidogrel
  • Drug Evaluation, Preclinical
  • Drug Therapy, Combination
  • Hemorrhage / chemically induced
  • Humans
  • Ischemia / prevention & control
  • Kidney Failure, Chronic / metabolism
  • Piperazines / adverse effects
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Platelet Aggregation Inhibitors / adverse effects
  • Platelet Aggregation Inhibitors / pharmacokinetics
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Aggregation Inhibitors / therapeutic use
  • Prasugrel Hydrochloride
  • Purinergic P2 Receptor Antagonists*
  • Randomized Controlled Trials as Topic
  • Receptors, Purinergic P2Y12
  • Thiophenes / adverse effects
  • Thiophenes / pharmacokinetics
  • Thiophenes / pharmacology*
  • Thiophenes / therapeutic use
  • Ticlopidine / analogs & derivatives
  • Ticlopidine / therapeutic use

Substances

  • P2RY12 protein, human
  • Piperazines
  • Platelet Aggregation Inhibitors
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2Y12
  • Thiophenes
  • Clopidogrel
  • Prasugrel Hydrochloride
  • Ticlopidine
  • Aspirin