title: Production, Quality Control and Pharmacokinetic Studies of (177)Lu-EDTMP for Human Bone Pain Palliation Therapy Trials.
abstract: Developing new bone pain palliation agents is a mandate in handling end-stage cancer patients around the world. Possibly, Lu-177 ethylenediaminetetramethylene phosphonic acid ((177)Lu-EDTMP) is a therapeutic agent which can be widely used in bone palliation therapy. In this study, (177)Lu-EDTMP complex was prepared successfully using synthesized EDTMP ligand and (177)LuCl3. Lu-177 chloride was obtained by thermal neutron irradiation (4 × 10(13) n.cm(-2)s(-1)) of natural Lu2O3 samples. Radiochemical purity of (177)Lu-EDTMP was determined by ITLC (more than 99%). Stability studies of the final preparations in the presence of human serum were performed. The biodistribution of (177)Lu-EDTMP and (177)LuCl3 in wild-type rats was studied by SPECT imaging. A comparative accumulation study for (177)Lu-EDTMP and (177)LuCl3 was performed for vital organs up to 7 days. The complex was obtained in high radiochemical purity (more than 99%). The complex was stable in vitro in presence of human serum as well as final formulation. Significant bone uptake (> 70%) was observed for the radiopharmaceutical. Due to better physical properties of Lu-177 compared to Sm-153 and acceptable biodistribution results of the compound, (177)Lu-EDTMP seemed to be an interesting new candidate for clinical trials for bone pain palliation therapy.
authors.affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors.forename: Ali
authors.initials: A
authors.lastname: Bahrami-Samani
authors.affiliation: Department of Radiation Medicine, Engineering Shahid Beheshti University, Tehran, Iran.
authors.forename: Akbar
authors.initials: A
authors.lastname: Anvari
authors.affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors.forename: Amir Reza
authors.initials: AR
authors.lastname: Jalilian
authors.affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors.forename: Simindokht
authors.initials: S
authors.lastname: Shirvani-Arani
authors.affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors.forename: Hassan
authors.initials: H
authors.lastname: Yousefnia
authors.affiliation: Department of Radiation Medicine, Engineering Shahid Beheshti University, Tehran, Iran.
authors.forename: Mahmoud Reza
authors.initials: MR
authors.lastname: Aghamiri
authors.affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Ghannadi-Maragheh
keywords: 177Lu-EDTMP; Biodistribution; Pharmacokinetic; Quality control.; Radiopharmaceutical