Production, quality control, biodistribution and imaging studies of 177Lu-PSMA-617 in breast adenocarcinoma model

摘要

177Lu-PSMA-617 therapeutic agent was prepared successfully under optimized condition of pH=4.5, molar ratio of metal to ligand 1:10, temperature of 95°C and 40 min reaction time. 177LuCl3 was obtained with specific activity of 70–80 GBq/mg by the thermal neutron irradiation (5×1013 n cm?2 s?1) of the enriched Lu2O3 (52% 176Lu) samples. The radionuclidic purity of 177LuCl3 (>99%) was checked by a HPGe detector. The radiochemical purities of 177LuCl3 solution and 177Lu-PSMA-617 compound (>98%) were checked by ITLC and HPLC techniques and stability studies were assayed in the presence of human serum. Biodistribution and imaging assessments in the breast adenocarcinoma-bearing mice showed a major accumulation of activity in the tumor and kidneys tissues, as the expression site of PSMA molecule and the main route of excretion, respectively.