Abstract: The incidence and mortality rate of prostate cancer (PCa) ranks sixth and seventh among Chinese men, and has become one of the fastest growing malignant tumors in the past decade. The authors reviewed the background, pharmacological profile, mechanism of action, and clinical research advancements of ¹⁷⁷Lu-prostate specific membrane antigen (PSMA)-I&T. ¹⁷⁷Lu-PSMA-I&T is a novel PCa therapeutic drug that targets PSMA and shows high affinity and specificity with PCa cells. Up to now, ¹⁷⁷Lu-PSMA-I&T has been widely applied in clinical research on tumors, which has shown promising clinical progress in PCa, salivary gland cancer, ceberal glioma and renal carcinoma. Therefore, the authors point out that ¹⁷⁷Lu-PSMA-I&T is expected to be a candidate drug for the treatment of PCa, which may optimize the current clinical therapeutic practices of PCa and holds vast application prospects for future clinical applications.