Optimal Use of Platelet Glycoprotein IIb/IIIa Receptor Antagonists in Patients Undergoing Percutaneous Coronary Interventions

• Published in: Drugs (New York, N.Y.) Vol. 71; no. 15; pp. 2009 - 2030
• Main Authors: Benjamin Starnes, H., Patel, Ankit A., Stouffer, George A.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.10.2011; Adis International; Wolters Kluwer Health, Inc; Springer Nature B.V
• Subjects: Abciximab; Acute coronary syndromes; Adenosine diphosphate; Angina pectoris; Antibodies, Monoclonal - therapeutic use; Aspirin; Biological and medical sciences; Blood platelets; Cardiology; Cardiovascular disease; Cardiovascular system; Clinical Trials as Topic; Coronary Disease - therapy; Coronary heart disease; Drug therapy; Glycoproteins; Health aspects; Heart attacks; Humans; Internal Medicine; Ligands; Medical sciences; Medicine; Medicine & Public Health; Mortality; Pharmacology. Drug treatments; Pharmacology/Toxicology; Pharmacotherapy; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - therapeutic use; Platelet Glycoprotein GPIIb-IIIa Complex - antagonists & inhibitors; Proteins; Review Article; Transluminal angioplasty; United States; Platelet Aggregation; Clopidogrel; Abciximab; Percutaneous Coronary Intervention; Acute Coronary Syndrome; Performance evaluation; Human; Drug; Glycoprotein IIbIIIa; Angioplasty; Treatment efficiency; Coronary artery; Pharmacotherapy; Instrumentation therapy; Monoclonal antibody; Review; Eptifibatide; Antiplatelet agent; Immunomodulator; Treatment; Tirofiban; Antithrombotic agent; Clinical trial; Combined treatment; Antagonist; Lamifiban; Biological receptor; Platelet glycoprotein IIb/IIIa receptor antagonist
• ISSN: 0012-6667; 1179-1950; 1179-1950
• DOI: 10.2165/11595010-000000000-00000

Discovery of the central role of platelets in the pathogenesis of acute coronary syndromes (ACS) and ischaemic complications of percutaneous coronary interventions (PCI) has led to the widespread use of oral and parenteral platelet inhibitors to treat these conditions. Glycoprotein (GP) IIb/IIIa (also known as α IIb β 3 ) receptors on the surface of platelets play an essential role in platelet aggregation and serve as a key mediator in the formation of arterial thrombus. When activated, GP IIb/IIIa receptors bind to fibrinogen, which serves as the ‘final common pathway’ in platelet aggregation. Of the numerous agents developed for modulating platelet activity, intravenous platelet GP IIb/IIIa receptor antagonists are the most potent. There are four agents in clinical use, including abciximab, eptifibatide, tirofiban and lamifiban, although lamifiban is not approved for use in the US. While all agents block fibrinogen binding to GP IIb/IIIa, they do so by different mechanisms. Abciximab is a humanized form of a murine monoclonal antibody directed against GP IIb/IIIa, eptifibatide is a synthetic, cyclic heptapeptide that contains a lysine-glycine-aspartic acid (KGD) sequence that mimics the arginine-glycine-aspartic acid (RGD) sequence found on GP IIb/IIIa, tirofiban is a non-peptide antagonist derived by optimization of the tyrosine analogue that structurally mimicks the RGD-containing loop of the disintegrin echistatin, and lamifiban is a synthetic, non-cyclic, non-peptide, low-molecular-weight compound. In clinical trials, use of these agents reduces ischaemic adverse cardiovascular events in patients with ACS undergoing PCI, but at a cost of increased bleeding.