Pharmacology and clinical trials of reversibly-binding P2Y12 inhibitors

Thromb Haemost. 2011 May:105 Suppl 1:S75-81. doi: 10.1160/THS10-12-0769. Epub 2011 Apr 11.

Abstract

The important role of the P2Y12 receptor in amplification of platelet activation and associated responses and the limitations associated with clopidogrel therapy have led to the development of novel inhibitors of this receptor. Three reversibly-binding P2Y12 inhibitors are in phase 3 development, ticagrelor, cangrelor and elinogrel. The pharmacology and clinical trial data for each of these inhibitors are discussed and compared with relevant data for the thienopyridines clopidogrel and prasugrel.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / pharmacology
  • Adenosine / therapeutic use
  • Adenosine Monophosphate / analogs & derivatives*
  • Adenosine Monophosphate / pharmacology
  • Adenosine Monophosphate / therapeutic use
  • Animals
  • Clinical Trials, Phase III as Topic
  • Clopidogrel
  • Humans
  • Piperazines / pharmacology
  • Piperazines / therapeutic use
  • Platelet Activation / drug effects
  • Prasugrel Hydrochloride
  • Protein Binding
  • Purinergic P2Y Receptor Antagonists / pharmacology*
  • Purinergic P2Y Receptor Antagonists / therapeutic use
  • Quinazolinones / pharmacology*
  • Quinazolinones / therapeutic use
  • Sulfonamides / pharmacology*
  • Sulfonamides / therapeutic use
  • Thiophenes / pharmacology
  • Thiophenes / therapeutic use
  • Thrombosis / drug therapy*
  • Thrombosis / physiopathology
  • Ticagrelor
  • Ticlopidine / analogs & derivatives
  • Ticlopidine / pharmacology
  • Ticlopidine / therapeutic use

Substances

  • Piperazines
  • Purinergic P2Y Receptor Antagonists
  • Quinazolinones
  • Sulfonamides
  • Thiophenes
  • Adenosine Monophosphate
  • cangrelor
  • elinogrel
  • Clopidogrel
  • Prasugrel Hydrochloride
  • Ticagrelor
  • Adenosine
  • Ticlopidine