Title:Effects Of Glycoprotein IIb/IIIa Antagonists: Anti Platelet Aggregation And Beyond
VOLUME: 17 ISSUE: 2
Author(s):Arturo Giordano, Giuseppe Musumeci, Anna D`Angelillo, Roberta Rossini, Giuseppe Biondi Zoccai, Stefano Messina, Enrico Coscioni, Simona Romano* and Maria Fiammetta Romano*
Affiliation:Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Universita di Napoli, Federico II, Via Pansini, 5. 80131, Napoli, Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Universita di Napoli, Federico II, Via Pansini, 5. 80131, Napoli
Keywords:Endothelium, GPIIbIIIa antagonists, healing, in stent thrombosis, integrin, platelet.
Abstract:Background: The use of inhibitors of glycoprotein IIb/IIIa (GPIIb/IIIa) has provided dramatic results in
terms of the prevention of acute stent thrombosis and a reduction in major adverse coronary events in patients subjected to percutaneous coronary intervention. GPIIb/IIIa or αIIbβ3 is a member of the β3 subfamily of integrins, which also includes αVβ3. GPIIb/IIIa functions as a receptor for fibrinogen and several adhesion proteins sharing an arginine-glycine-aspartic acid (RGD) sequence. GPIIb/IIIa antagonists, through blockade of the receptor, prevent platelet aggregation. Among the three GPIIb/IIIa antagonists used in therapy, abciximab is an anti-β3 monoclonal antibody, while tirofiban and eptifibatide mimic the binding sequence of the fibrinogen ligand. Although
antiplatelet aggregation represents the central function of GPIIb/IIIa inhibitors, further actions have been documented for these
compounds.
Objective: The aim of the present article is to review the structures and functions of GPIIb/IIIa antagonists and to highlight the clinical
outcomes and results of randomized trials with these compounds. Hypotheses on the unexplored potential of GPIIb/IIIa antagonists will
be put forward.
Conclusion: GPIIb/IIIa inhibitors were developed to prevent platelet aggregation, however, these compounds can exert further biological
functions, both platelet- and non-platelet-related. Large-scale studies comparing the efficacy and safety of GPIIb/IIIa antagonists are
lacking. More insights into the functions of these compounds may lead to generation of novel small molecules able to antagonize platelet
aggregation while promoting vascular repair.
