Preliminary Dosimetric Evaluation of a New Therapeutic 177Lu Complex for Human Based on Biodistribution Data in Rats

Abstract—[Tris (1,10-phenanthroline) lanthanum(III)] trithiocyanate is a new compound that has shown high ability for stopping the synthesis of DNA and also acting as a photosensitizer. Nowadays, the radiation dose assessment resource (RADAR) method is known as the most common method for absorbed dose calculation. 177Lu was produced by (n, gamma) reaction in a research reactor. 177Lu-PL3 was prepared in the optimized condition. The radiochemical yield was checked by ITLC method. The biodistribution of the complex was investigated by intravenously injection to wild-type rats via their tail veins. In this study, the absorbed dose of 177Lu-PL3 to human organs was estimated by RADAR method. 177Lu was prepared with a specific activity of 2.6-3 GBq.mg-1 and radionuclide purity of 99.98 %. Final preparation of the radiolabelled complex showed high radiochemical purity of > 99%. The results show that liver and spleen have received the highest absorbed dose of 1.051 and 0.441 mSv/MBq, respectively. The absorbed dose values for these two dose-limiting tissues suggest more biological studies special in tumor-bearing animals.

Human Absorbed Dose Estimation of a New IN-111 Imaging Agent Based on Rat Data

The measurement of organ radiation exposure dose is one of the most important steps to be taken initially, for developing a new radiopharmaceutical. In this study, the dosimetric studies of a novel agent for SPECT-imaging of the bone metastasis, 111In- 1,4,7,10-tetraazacyclododecane-1,4,7,10 tetraethylene phosphonic acid (111In-DOTMP) complex, have been carried out to estimate the dose in human organs based on the data derived from rats. The radiolabeled complex was prepared with high radiochemical purity in the optimal conditions. Biodistribution studies of the complex was investigated in the male Syrian rats at selected times after injection (2, 4, 24 and 48 h). The human absorbed dose estimation of the complex was made based on data derived from the rats by the radiation absorbed dose assessment resource (RADAR) method. 111In-DOTMP complex was prepared with high radiochemical purity of >99% (ITLC). Total body effective absorbed dose for 111In- DOTMP was 0.061 mSv/MBq. This value is comparable to the other 111In clinically used complexes. The results show that the dose with respect to the critical organs is satisfactory within the acceptable range for diagnostic nuclear medicine procedures. Generally, 111In- DOTMP has interesting characteristics and can be considered as a viable agent for SPECT-imaging of the bone metastasis in the near future.