In Vivo Platelet Detection Using a Glycoprotein IIb/IIIa-Targeted Near-Infrared Fluorescence Imaging Probe.

Platelets play a prominent role in multiple diseases, in particular arterial and venous thrombosis and also in atherosclerosis and cancer. To advance the in vivo study of the biological activity of this cell type from a basic experimental focus to a clinical focus, new translatable platelet-specific molecular imaging agents are required. Herein, we report the development of a near-infrared fluorescence probe based upon tirofiban, a clinically approved small-molecule glycoprotein IIb/IIIa inhibitor (GPIIb/IIIa). Through in vitro experiments with human platelets and in vivo ones in a murine model of deep-vein thrombosis, we demonstrate the avidity of the generated probe for activated platelets, with the added benefit of a short blood half-life, thereby enabling rapid in vivo visualization within the vasculature.