Effects Of Glycoprotein IIb/IIIa Antagonists: Anti Platelet Aggregation And Beyond

Author(s): Arturo Giordano, Giuseppe Musumeci, Anna D`Angelillo, Roberta Rossini, Giuseppe Biondi Zoccai, Stefano Messina, Enrico Coscioni, Simona Romano*, Maria Fiammetta Romano*

Journal Name: Current Drug Metabolism

Volume 17 , Issue 2 , 2016

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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.

Keywords: Endothelium, GPIIbIIIa antagonists, healing, in stent thrombosis, integrin, platelet.

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Article Details

Year: 2016
Published on: 14 January, 2016
Page: [194 - 203]
Pages: 10
DOI: 10.2174/1389200217666151211121112
Price: $65

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