Synthesis and evaluation of 111In-labeled d-glucose as a potential SPECT imaging agent

The purpose of this study was to develop an efficient synthetic method for labeling d-Glucosamine with indium-111 (111In), and to investigate the imaging properties of the resulting radiotracer in MDA-MB-468 xenograft models using single-photon emission computed tomography (SPECT). The precursor compound, 2-(4-Isothiocyanato benzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-deoxyglucosone (DOTA-DG), was synthesized from 2-d-Glucosamine. DOTA-DG was labeled with 111In within 20 min. The labeling efficiency and radiochemical purity of 111In-DOTA-DG were >95 and >96 % as determined by radio-HPLC. SPECT imaging studies were performed using nude mice bearing MDA-MB-468 mammary tumors after intravenous injection of at a dose of 1.11 MBq (0.1 mL) 111In-DOTA-DG. Tumors were clearly delineated by SPECT imaging at 120 min after injection.