Development of 153Sm/177Lu-EDTMP as a possible therapeutic complex

Targeted radionuclide therapy (TRT) has been demonstrated to be an effective therapeutic tool in patients with disseminated bone metastasis. TRT is generally performed with a single radionuclide. In this study we investigated the feasibility of combined TRT with a high-energy beta emitter (153Sm) and a low energy beta emitter (177Lu) in wistar rats.
The cocktail complex of 153Sm/177Lu-EDTMP was prepared. To determine the effect of metal-to-ligand (Me:EDTMP) molar ratio on labeling yield, several complex were analyzed after changing Me:EDTMP molar ratio from 1:1 to 1:50. 153Sm/177Lu-EDTMP was administered intravenously through the tail vein of wistar rats. Biodistribution data were collected at 2 hours to 7 day post injection and scintigraphic images were taken at 24 hours and 1, 2 week after administration of radiopharmaceutical.
The results revealed high skeletal uptake (3.5% and 3.4% ID/g at 24 hours post injection for 153Sm and 177Lu, respectively) with rapid blood clearance and minimal uptake in any of the major organs. Scintigraphic images verified high skeletal uptake.
Our results indicate that the combination of 153Sm and 177Lu is feasible and safe. This study suggests that the combination of different radionuclides with different radiation energies and half-life, such as 153Sm and 177Lu, could be advantageous in patients with tumoral lesions of different sizes.