Conventional therapy (such as palliative surgery, experimental local therapy, external radiotherapy, endocrine therapy and chemotherapy) has limited effect on the prognosis and quality of life in patients with metastatic castration-resistant prostate cancer (mCRPC). Radioligand therapy (RLT) with prostate-specific membrane antigen (PSMA) targeted probe is expected to change the situation (short survival and poor quality of life in mCRPC patients). ¹⁷⁷Lutetium labelled PSMA targeted ligand PSMA-617 (¹⁷⁷Lu-PSMA-617) has excellent physical and chemical properties and pharmacokinetic properties. Compared with other radionuclide labelled probes, we have accumulated more clinical research data and experience on ¹⁷⁷Lu-PSMA-617. High efficacy, safety and easy availability, endowed it with high clinical value and application prospects in spite of several limitations. Although research on RLT with ¹⁷⁷Lu-PSMA-617 is still based on small sample size and single center research at present, it is expected to become an extension and supplement to clinical conventional therapy for mCRPC patients with the accumulation of big data of global research.