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Tirofiban is a potent nonpeptide glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; IC50 = 5 nM in a radioligand binding assay).1 It inhibits GPIIb/IIIa-dependent platelet aggregation with an IC50 value of 11 nM. Tirofiban is selective for platelet GPIIb/IIIa, only inhibiting human umbilical vein endothelial cell (HUVEC) attachment to microtiter plates containing fibrinogen (Fg), human vitronectin (Vn), or human fibronectin (Fn) at concentrations >10,000-fold above the IC50 for platelet aggregation. Tirofiban (300 and 1,000 μg/kg per minute, i.v.) prevents occlusive thrombosis and reduces thrombus mass in a canine model of electrically-induced coronary artery occlusive thrombosis.2 Formulations containing tirofiban have been used to prevent thrombotic occlusion associated with coronary angioplasty.3
WARNING This product is not for human or veterinary use.
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2. Nonpeptide glycoprotein IIb/IIIa inhibitors. 5. Antithrombotic effects of MK-
3. Effects of platelet glycoprotein IIb/IIIa blockade with tirofiban on adverse cardiac events in patients with unstable angina or acute myocardial infarction undergoing coronary angioplasty. Circulation 96(5), 1445-1453 (1997).