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]LuCl[3]. Lu-177 chloride was obtained by thermal neutron irradiation [4 _ 10[13] n.cm[-2]s[-1]] of natural Lu[2]O[3] 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]LuCl[3] in wild-type rats was studied by SPECT imaging. A comparative accumulation study for [177]Lu-EDTMP and [177]LuCl[3] 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