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

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*Maria Fiammetta Romano*

Affiliation:

• Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Universita di Napoli, Federico II, Via Pansini, 5. 80131, Napoli,Italy

• Dipartimento di Medicina Molecolare e Biotecnologie Mediche, Universita di Napoli, Federico II, Via Pansini, 5. 80131, Napoli,Italy

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.

Cite this article as:

Giordano Arturo , Musumeci Giuseppe , D`Angelillo Anna , Rossini Roberta , Zoccai Biondi Giuseppe , Messina Stefano , Coscioni Enrico , Romano Simona *, Romano Fiammetta Maria *, Effects Of Glycoprotein IIb/IIIa Antagonists: Anti Platelet Aggregation And Beyond, Current Drug Metabolism 2016; 17 (2) . https://dx.doi.org/10.2174/1389200217666151211121112