Novel 99mTc-Labeled Glucose Derivative for Single Photon Emission Computed Tomography: A Promising Tumor Imaging Agent

In this study, a D-glucosamine derivative with an isonitrile group (CNSDG) was synthesized and it was chosen to coordinate with Tc-99m for preparing Tc-99m-CNSDG. Tc-99m-CNSDG could be readily obtained with high radiochemical purity (>95%) and had great in vitro stability and metabolic stability in urine. The radiotracer demonstrated a positive response to the administration of glucose and insulin in S180 and A549 tumor cells in vitro, suggesting the mechanism of Tc-99m-CNSDG into tumor cells was related to glucose transporters. Biodistribution studies in mice bearing AS49 xenografts showed Tc-99m-CNSDG had a high tumor uptake and high tumor-to-background ratios. SPECT/CT images further supported its ability for tumor imaging. As a cheap, conveniently made and widely available probe, Tc-99m-CNSDG would become a potential working horse and be a breakthrough in Tc-99m-labeled radiopharmaceuticals for tumor detection.