αIIbβ3 (GPIIb-IIIa) antagonists

Platelets play a key role in thrombosis and hemostasis, especially during an acute coronary syndrome and in patients undergoing percutaneous coronary intervention. Associated adverse cardiovascular events from normal platelet function can be mitigated via adequate platelet inhibition. Glycoprotein IIb-IIIa (αIIbβ3) antagonists were first introduced to the market with the intent of being potent, intravenous, antiplatelet agents with a quick onset of action. These agents have been the centerpiece of multiple well conducted investigations over the last several decades. In this chapter, we briefly discuss the pharmacological mechanism and subtle differences between the three currently available intravenous glycoprotein IIb-IIIa antagonists: abciximab, eptifibatide, and tirofiban. Furthermore, we present data from landmark clinical trials highlighting the efficacy and safety of these agents in various clinical scenarios. Lastly, we present a comparison between these agents and other antiplatelet drugs as well as the role of these agents in our modern-day clinical practice.