The purpose of the present work was to introduce ¹⁴¹Ce-EDTMP as a novel potential future pain palliative agent to patients suffering from disseminated skeletal metastases and diagnostic imaging radioisotope as well. Cerium-141 [T_1/2 = 32.501 days, E_β (max) = 0.580 (29.8%) and 0.435(70.2%) MeV, E_γ = 145.44 (48.2%) keV] possesses radionuclidic properties suitable for use in palliative therapy of bone metastases. ¹⁴¹Ce also has gamma energy of 145.44 keV, which resembles that of ^99mTc. Therefore, the energy window is adjustable on the Tc-99m energy because of imaging studies. ¹⁴¹Ce can be produced through a relatively easy route that involves thermal neutron bombardment on natural CeO₂ in medium flux research reactors (4–5×10¹³ neutrons/cm²·s). The requirement for an enriched target does not arise. Ethylenediamine (tetramethylene phosphonic acid) (EDTMP) was synthesized and radiolabeled with ¹⁴¹Ce. The experimental parameters were optimized to achieve maximum yields (>99%). The radiochemical purity of ¹⁴¹Ce-EDTMP was evaluated by radio-thin layer chromatography. The stability of the prepared formulation was monitored for one week at room temperature, and results showed that the preparation was stable during this period (>99%). Biodistribution studies of the complexes carried out in wild-type rats exhibited significant bone uptake with rapid clearance from blood. The images showed high uptake of complex in bone after 72h and 2 weeks clearly. The percentage injected dose per gram of tissue (%ID/g) for each organ or tissue was calculated. The results show significant bone uptake with rapid clearance from blood. The properties of produced ¹⁴¹Ce-EDTMP suggest applying a new efficient bone pain palliative therapeutic agent to overcome metastatic bone pains.