Prasugrel: a novel platelet ADP P2Y(12) receptor antagonist.
Novel adenosine diphosphate (ADP) P2Y(12) antagonists such as 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. Pre-clinical and early phase clinical studies have shown prasugrel to be characterized by more potent antiplatelet effects, lower inter-individual variability in platelet response, and faster onset of activity compared to clopidogrel. Recent findings from large-scale phase-III testing show prasugrel to be more efficacious in preventing ischemic events in acute coronary syndrome patients 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.
Mousa
Shaker A
SA
Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Rensselaer, NY, USA.
Jeske
Walter P
WP
Fareed
Jawed
J
D002986:Clinical Trials as Topic; D006801:Humans; D007676:Kidney Failure, Chronic / Q000188:drug therapy / Q000378:metabolism; D010879:Piperazines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D000068799:Prasugrel Hydrochloride; D058919:Purinergic P2 Receptor Antagonists; D013876:Thiophenes / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use
D010879:Piperazines; D058919:Purinergic P2 Receptor Antagonists; D013876:Thiophenes; D000068799:Prasugrel Hydrochloride