The GPIIb/IIIa inhibitors were the first clinically used anti-integrin therapeutics. They opened the gate to a rapidly developing area of anti-integrin targeting as a therapeutic approach to many diseases. The use of GPIIb/IIIa inhibitors in interventional cardiology is widespread and still increasing, as is the number of percutaneous coronary interventions. There seems to be a class effect of GPIIb/IIIa inhibitors in percutaneous coronary intervention, but there are major differences in the pharmacokinetics and pharmacodynamics of these agents. Currently clinically approved for parenteral use are the Fab fragment abciximab (ReoPro, Lilly) and the small-molecule GPIIb/IIIa inhibitors eptifibatide (Integrilin, Millennium/Schering-Plough) and tirofiban (Aggrastat, Merck). This review focuses on the different pharmacological properties of these agents and summarizes present and future therapeutic use of GPIIb/IIIa inhibitors in cardiovascular and other vascular diseases.