Tirofiban is an antagonist of the gpIIb/IIIa receptor. It was developed as an intravenous agent for rapid, potent and reversible inhibition of platelet aggregation. It produces dose-related inhibition of aggregation. Its efficacy has been demonstrated in disease states associated with intravascular thrombus formation, such as occurs with unstable angina pectoris, non-Q-wave myocardial infarction and during percutaneous coronary interventions. This review describes the pharmacokinetics and pharmacodynamics of tirofiban in normal volunteers and in patients with coronary artery disease, including patients with renal or hepatic insufficiency, as well as the results of the phase III program that has studied the efficacy and safety profile of the drug. Modalities for its clinical use are also discussed.