Among the radiopharmaceuticals harnessed for palliation of bone pain in osseous metastases patients, ¹⁷⁷Lu labeled phosphonates such as EDTMP (Ethylene diamine tetramethylene phosphonic acid) as well as DOTMP (1,4,7,10-tetraazacyclo-dodecane-1,4,7,10 tetraethylene phosphonic acid) and ¹⁸⁸Re-labeled HEDP (1,1-hydroxyethylene diphosphonic acid) seem to be the most favorable for treatment of small and medium/large size bone lesions, respectively. A comparative assessment of ¹⁷⁷Lu-EDTMP, ¹⁷⁷Lu-DOTMP and ¹⁸⁸Re-HEDP in osteosarcoma tumor cell line was carried out to evaluate their relative efficacy. It was found that ¹⁸⁸Re-HEDP is more potent in induction of cell toxicity and apoptosis compared to the ¹⁷⁷Lu-EDTMP and ¹⁷⁷Lu-DOTMP, thus ¹⁸⁸Re-HEDP might have great clinical significance.