摘要转移性去势抵抗性前列腺癌（mCRPC）是前列腺癌的终末阶段，该阶段的患者往往预后较差且治疗选择有限。前列腺特异性膜抗原（PSMA）是一种Ⅱ型跨膜糖蛋白，在大多数前列腺癌细胞膜表面高表达，其表达水平与肿瘤侵袭、转移能力显著相关，已成为前列腺癌精准诊疗领域的重要靶点。近年来，靶向PSMA的放射性配体疗法（RLT）发展迅速， 177Lu-PSMA-617可以精准靶向前列腺癌细胞，递送镥-177（ 177Lu）释放的β射线，诱导肿瘤细胞DNA链断裂从而杀伤肿瘤细胞，在mCRPC阶段的疗效和安全性已得到高级别证据证实，获得了国内外前列腺癌权威指南的一致推荐。本文综述了以 177Lu-PSMA-617为代表的RLT的作用机制、临床数据和相关研究进展，为临床实践和研究探索提供参考。

abstractsMetastatic castration-resistant prostate cancer（mCRPC）is the terminal stage of prostate cancer，often associated with poor prognosis and limited treatment options. Prostate-specific membrane antigen（PSMA），a type Ⅱ transmembrane glycoprotein，is highly expressed on the surface of most prostate cancer cells. The expression level of PSMA is significantly associated with tumor migration and invasion，making it a critical target in the diagnosis and treatment of prostate cancer. In recent years，radioligand therapy（RLT）targeting PSMA has rapidly advanced. 177Lu-PSMA-617 delivers beta radiation from 177Lu to selectively kill prostate cancer cells by inducing DNA damage. 177Lu-PSMA-617 has demonstrated promising efficacy and safety in mCRPC，gaining widespread endorsement in global prostate cancer guidelines. This review summarizes the mechanism，clinical evidence，and progress of RLT，with a focus on 177Lu-PSMA-617，offering insights for clinical practice and research.