Evaluation of tumor uptake and bio-distribution of 99mTc-labeled 1-thio-β-D-glucose and 5-thio-D-glucose in vivo

Abstract

Background To investigate the capacity of 99mTc-labeled 1-thio-β-D-glucose (1-TG) and 5-thio-D-glucose (5-TG) to act as a marker for glucose consumption in tumor cells in vivo as well as to evaluate the biodistribution of 1-TG and 5-TG. We investigated the biodistribution, including tumor uptake, of 1-TG and 5-TG at various time points after injection (0.5, 2 and 4 h) in human colorectal carcinoma and human lung adenocarcinoma (HCT-116, A549) xenograft bearing nude mice (N=4 per tracer and time point). Results: In vivo biodistribution studies revealed a maximum tumor-to-muscle ratio of 4.22 ± 2.7 and 2.2 ± 1.3 (HCT-116) and of 3.2 ± 1.1 and 4.1 ± 1.3 (A549) for 1-TG and 5-TG, respectively, with a peak at 4 hours for 1-TG and 5-TG. Biodistribution revealed a high uptake in kidneys and liver for 1-TG and in the lung, liver, and kidneys for 5-TG. Conclusions: 1-TG and 5-TG showed an insufficient tumor uptake for diagnostic use in human colorectal carcinoma and human lung adenocarcinoma xenograft model.