Painful metastatic bone involvement is common in advanced stages of many cancers. Between available radionuclides for bone pain palliation, no consensus has been reached on lutetium ethylenediaminetetramethylene phosphonate (Lu-EDTMP) administration in this milieu. The aim of this study is to evaluate the treatment efficacy, safety profile, and toxicities of Lu-EDTMP in patients with metastatic bone involvement, according to the published literature. A comprehensive literature search of PubMed/MEDLINE, Scopus, and Google Scholar databases was carried out to retrieve pertinent articles published until January 2019, concerning the clinical efficacy and safety of Lu-EDTMP for bone pain palliative purposes. Eight studies (172 patients) were included. This analysis revealed statistically significant effect of Lu-EDTMP therapy on the visual analog score (4.84% (95% CI: 3.88-5.81;  < 0.001), bone palliative pain response (84%, 95% CI: 75%-90%;  < 0.001), and Karnofsky performance status (21%, 95% CI: 18%-24%;  < 0.001) overall (as well as in the high-dose and low-dose subgroups). Complete palliative pain response to treatment was observed in 32% (95% CI: 16%-53%) of patients receiving Lu-EDTMP. Anemia was found to be the most common hematologic toxicity imposed by this therapeutic approach (grade I/II anemia in 24% (95% CI: 14%-38%;  < 0.001) and grade III/IV anemia in 19% (95% CI: 12%-28%;  < 0.001)). Lu-EDTMP seems to have comparable efficacy and safety profile as that of the frequently administered radiopharmaceuticals for bone palliation. Therefore, this agent can be a good option for bone pain palliative purposes, in case of limited access to other bone palliative radiopharmaceuticals.