title: Pharmacology and clinical trials of reversibly-binding P2Y12 inhibitors.
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.
authors.affiliation: Department of Cardiovascular Science, University of Sheffield, Beech Hill Road, Sheffield, UK. r.f.storey@sheffield.ac.uk
authors.forename: Robert F
authors.initials: RF
authors.lastname: Storey
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D000249:Adenosine Monophosphate / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D017326:Clinical Trials, Phase III as Topic; D000077144:Clopidogrel; D006801:Humans; D010879:Piperazines / Q000494:pharmacology / Q000627:therapeutic use; D015539:Platelet Activation / Q000187:drug effects; D000068799:Prasugrel Hydrochloride; D011485:Protein Binding; D058921:Purinergic P2Y Receptor Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D052999:Quinazolinones / Q000494:pharmacology* / Q000627:therapeutic use; D013449:Sulfonamides / Q000494:pharmacology* / Q000627:therapeutic use; D013876:Thiophenes / Q000494:pharmacology / Q000627:therapeutic use; D013927:Thrombosis / Q000188:drug therapy* / Q000503:physiopathology; D000077486:Ticagrelor; D013988:Ticlopidine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D010879:Piperazines; D058921:Purinergic P2Y Receptor Antagonists; D052999:Quinazolinones; D013449:Sulfonamides; D013876:Thiophenes; D000249:Adenosine Monophosphate; C117446:cangrelor; C549473:elinogrel; D000077144:Clopidogrel; D000068799:Prasugrel Hydrochloride; D000077486:Ticagrelor; D000241:Adenosine; D013988:Ticlopidine