Ticagrelor.
Coronary artery disease (CAD) is the single leading cause of death in the U.S. Therapies for CAD have been developed to inhibit platelet aggregation underlying atherogenesis. Clinical benefit has been shown with antagonists of the P2Y(12) receptor, such as clopidogrel. However, concerns over patient resistance to treatment and relatively slow onset and offset of action have indicated the need for further pharmacotherapeutic development. Ticagrelor (formally AZD-6140) is a novel, reversible oral P2Y(12) antagonist developed by AstraZeneca. In vitro and in vivo studies have confirmed that ticagrelor provides rapid, enhanced and maintained antiplatelet effects. These findings have translated to clinical trial investigations with further evidence for a significantly reduced mortality rate associated with cardiovascular events, myocardial infarction (MI) or stroke, and a favourable safety profile. Key clinical trials to date include the DISPERSE, DISPERSE2, PLATO, ONSET/OFFSET and RESPOND. Ticagrelor has been put forward for approval to the European Medical Agency (EMEA) and the Food and Drug Administration (FDA) as an investigational oral antiplatelet treatment for the reduction of major adverse cardiac events in patients with acute coronary syndrome.
Davies
Shelley L
SL
Institute of Science and the Environment, University of Worcester, Worcester, UK. s.davies@worc.ac.uk
D054058:Acute Coronary Syndrome / Q000188:drug therapy / Q000503:physiopathology; D000241:Adenosine / Q000031:analogs & derivatives* / Q000494:pharmacology; D000284:Administration, Oral; D000818:Animals; D002986:Clinical Trials as Topic; D003324:Coronary Artery Disease / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D058919:Purinergic P2 Receptor Antagonists; D058925:Receptors, Purinergic P2Y12; D000077486:Ticagrelor
C548576:P2RY12 protein, human; D010975:Platelet Aggregation Inhibitors; D058919:Purinergic P2 Receptor Antagonists; D058925:Receptors, Purinergic P2Y12; D000077486:Ticagrelor; D000241:Adenosine