Objective: The purpose of this study was to explore the potential use of 177 Lu-diethylenetriamine penta-acetic acid-deoxyglucose (177 Lu-DTPA-DG) as a radiopharmaceutical for hepatic tumor treatment. Methods: Lutetium-177 (177 Lu) was labeled with DTPA-DG by adding 2 mCi 177 LuCl 3 to 0.05 mg DTPA-DG (pH 5-6) at room temperature for 1 h. The quality of the 177 Lu-DTPA-DG solutions was determined by thinlayer chromatography and high-performance liquid chromatography. Cellular uptake studies with 18 Ffluorodeoxyglucose (FDG), 177 Lu-DTPA-DG and 177 Lu-DTPA and a blocking study with 1.0 mg d-glucose were performed. Biodistribution, imaging, and radiotherapy studies of 177 Lu-DTPA-DG were performed with the SMMC-7721 model. Results: 177 Lu-DTPA-DG had a high radiochemical purity (>97%). The cellular uptake of 177 Lu-DTPA-DG was much higher than that of the 177 Lu-DTPA. The biodistribution of 177 Lu-DTPA-DG demonstrated that the complex accumulated in the tumor with high tumor/blood and tumor/muscle ratios. The tumors in mice in the 177 Lu-DTPA-DG group clearly displayed the high uptake of 177 Lu-DTPA-DG. After radiotherapy with 177 Lu-DTPA-DG, tumor growth decreased, and the overall survival was longer than that in the 177 LuCl 3 group (268.58-17.96 mm 3 vs. 507.43-55.72 mm 3 , p = 0.002) and the normal saline group (268.58-17.96 mm 3 vs. 483.68-27.51 mm 3 , p < 0.05). Conclusions: This preliminary study suggests that 177 Lu-DTPA-DG has the potential to become a liver radiopharmaceutical agent and should be further investigated.