Oral inhibitors of platelet membrane receptor glycoprotein IIb/IIIa in clinical cardiology: issues and opportunities.
The feedback amplification loop in the progress of medicine, from basic findings and clinical observations to hypothesis generation and new research, is presently particularly dynamic in acute coronary syndromes. As the role of thrombosis formation in etiopathology of these syndromes has emerged, antithrombotic therapy has become standard practice. Numerous trials with antiplatelet drugs and meta-analyses of these trials have established the efficacy of aspirin, launching new research in platelet physiology, understanding of pathophysiology, and therapy. Recognition of the role of glycoprotein IIb/IIIa receptor in health and disease and of its dynamic and ligands lead to production of a monoclonal antibody against the receptor, which has become the first anti-integrin therapy approved for clinical use. Synthetic compounds were subsequently produced containing the specific arginine-glycine-aspartic acid (RGD) sequence for fibrinogen binding to the receptor. Inhibitors are now available for oral use, allowing prolonged blockade of the receptor and opportunities for new research and hypothesis generation as well as better patient care. This supplement to the American Heart Journal summarizes a workshop whose goal was to generate a discussion among fundamentalists and clinicians on methods for monitoring platelet function with these drugs and investigation of consequences of chronic receptor occupancy.
Théroux
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Department of Medicine, Montreal Heart Institute and University of Montreal, Quebec, Canada.
D000284:Administration, Oral; D002309:Cardiology / Q000379:methods*; D002561:Cerebrovascular Disorders / Q000517:prevention & control; D002986:Clinical Trials as Topic; D003327:Coronary Disease / Q000188:drug therapy; D006801:Humans; D002546:Ischemic Attack, Transient / Q000188:drug therapy; D009203:Myocardial Infarction / Q000517:prevention & control; D017202:Myocardial Ischemia / Q000517:prevention & control; D010975:Platelet Aggregation Inhibitors / Q000627:therapeutic use; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors*
D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex