Tirofiban is a small-molecule, nonpeptide tyrosine derivative. Though similar to abciximab in that it has a high specificity and affinity for the glycoprotein (GP)IIb/IIIa receptor, tirofiban dissociates from the GPIIb/IIIa receptor more rapidly than abciximab. Additionally, it is reversed within hours after the completion of the infusion, whereas abciximab rather binds irreversibly resulting in a considerably longer effect. GPIIb/IIIa blockers have been initially developed in the preclopidogrel era, and therefore, much of the evidence generated through their use may not be applicable today. Yet, there is today emerging evidence that inhibition of P2Y12 and GPIIb/IIIa receptors on the platelet via tirofiban may actually potentially play a complementary role in further reducing the incidence of ischemic events in patients with acute coronary syndromes (ACS) encompassing both non-ST-segment-elevation ACS syndromes (NSTE-ACS) and STE-ACS.