Heightened platelet activity is pivotal in the thrombosis underlying acute coronary syndrome (ACS). The glycoprotein IIb/IIIa inhibitor tirofiban is a powerful platelet inhibitor with demonstrated efficacy and safety across the spectrum of ACS. Despite tirofiban's impact on the platelet compared with placebo, only an excess in minor and importantly not major bleeding has been observed. Thrombocytopenia with tirofiban seems to be extremely rare and immediately reversible on infusion discontinuation.The review includes the rationale for potent antiplatelet therapy in the management of ACS, particularly patients at high risk for ischemic complications. Additionally, it provides an overview of tirofiban's pharmacology and summary of the clinical efficacy and safety data of two dosing regimens.The reader will gain a perspective on the efficacy and safety data from the key trials of tirofiban.Tirofiban is safe and effective in patients with ACS. The single bolus dose regimen produces potent platelet inhibition resulting in significant improvement in clinical events over placebo when initiated just prior to percutaneous coronary intervention and at first medical contact. When compared with abciximab, tirofiban demonstrates similar efficacy though significantly lower rates of thrombocytopenia.