针对转移性去势抵抗性前列腺癌（mCRPC）患者的特异性前列腺膜抗原（PSMA）靶向放射性配基治疗（PRLT）在肿瘤学界引起了极大的关注。多项文献报道，在低毒性副作用的情况下，PRLT展现出良好的疗效和生存益处。本文讨论了177Lu-PSMA-617的适应症，患者准备，剂量给予，治疗后成像，剂量测定以及副作用配置文件。我们还讨论了有关PRLT的前瞻性研究，重要的回顾性研究，荟萃分析，临床试验以及正在进行的重要临床试验的结果。我们还阐述了我们自己的经验和对PRLT的未来展望。 在PRLT中，PSMA-617和PSMA-I＆T分子在晚期前列腺癌的治疗策略中具有重大革命性意义，多篇发表的文章表明，177Lu-PSMA-617具有良好的疗效和卓越的安全性。大多数mCRPC患者在177Lu-PSMA-617 PRLT后发现生活质量和生存率有所提高。相比于年龄、症状、肝脏、脑和骨骼转移，只有淋巴结转移，PSMA高表达病变且没有不符合FDG-avid病变的特征的患者表现出更长的生存期。多西他赛和卡巴噻吨是mCRPC患者的已批准治疗方法。177Lu-PSMA-617已被批准作为第三线全身治疗方法，适用于对雄激素受体通路抑制剂和多西他赛治疗无反应的mCRPC患者。PRLT是卡巴噻吨（第三线全身治疗方法）的一种安全有效的替代疗法，但其成本较高。177Lu-PSMA-617可能是mCRPC患者的一种更有效的治疗选择，可作为一线或联合治疗，并可能是治疗转移性激素敏感前列腺癌（mHSPC）患者的有用治疗选择。目前正在进行多项有关PRLT的临床研究和临床试验。将来，这些试验的结果将有助于发展前列腺癌患者的治疗策略。

The prostate-specific membrane antigen (PSMA) targeted radioligand therapy (PRLT) for the treatment of metastatic castration-resistant prostate cancer (mCRPC) patients has generated significant interest among the oncologic community, with several publications documenting good response rates and survival benefits with low toxicity profiles.Indications, patient preparation, dose administration, post-treatment imaging, dosimetry, and side effect profiles of 177Lu-PSMA-617 are discussed in this article. We also discuss results from prospective studies, major retrospective studies, meta-analyses, clinical trials, and mentioned major ongoing clinical trials on PRLT. We have also portrayed our own experiences and future perspectives on PRLT.For PRLT, PSMA-617 and PSMA-I&T molecules have revolutionized the theranostic approach in the management of advanced prostate cancer, with solid backing from several published articles showing favorable outcomes and an excellent safety profile of 177Lu-PSMA-617. Improvement in quality of life and survival was seen in the majority of mCRPC patients after 177Lu-PSMA-617 PRLT. Patients with features of good performance or asymptomatic status, only lymph node metastases, high PSMA-expressing lesions with no discordant FDG-avid lesions demonstrate longer survival as compared to patients with features of poor performance status, symptomatic, hepatic, brain, and skeletal metastases, discordant PSMA-avid and FDG-avid lesions, respectively. Docetaxel and cabazitaxel are approved treatments for mCRPC patients. 177Lu-PSMA-617 is approved as a third-line systemic treatment for mCRPC patients with failure to respond to androgen receptor pathway inhibitors and docetaxel therapy. PRLT is a safe and effective alternative to cabazitaxel (third-line systemic treatment), but it has a higher cost. 177Lu-PSMA-617 could be a more efficient therapeutic option for mCRPC patients as first-line or combined therapy, and it may be a useful therapeutic option for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC) patients. Several clinical studies and clinical trials on PRLT are currently underway. In the future, the results of these trials will be helpful in evolving treatment strategies for prostate cancer patients.