Department of Nuclear Medicine, West China Hospital, Sichuan University, 610041, Chengdu, China.
Department of Biochemistry & Molecular Biology, West China School of Basic Medical Sciences & Forensic Medicine, Sichuan University, Chengdu, 610041, China.
Curr Top Med Chem. 2019;19(1):33-56. doi: 10.2174/1568026619666190201100739.
Prostate cancer (PCa) is the most common sex-related malignancy with high mortality in men worldwide. Prostate-specific membrane antigen (PSMA) is overexpressed on the surface of most prostate tumor cells and considered a valuable target for both diagnosis and therapy of prostate cancer. A series of radiolabeled agents have been developed based on the featured PSMA ligands in the previous decade and have demonstrated promising outcomes in clinical research of primary and recurrent PCa. Furthermore, the inspiring response and safety of lutetium-177-PSMA-617 (177Lu-PSMA-617) radiotherapy represent the potential for expanded therapeutic options for metastatic castration-resistant PCa. Retrospective cohort studies have revealed that radiolabeled PSMA agents are the mainstays of the current success, especially in detecting prostate cancer with metastasis and biochemical recurrence.
This review is intended to present a comprehensive overview of the current literature on PSMA ligand-based agents for both radionuclide imaging and therapeutic approaches, with a focus on those that have been clinically adopted.
PSMA-based diagnosis and therapy hold great promise for improving the clinical management of prostate cancer.
前列腺癌（PCa）是全球男性中最常见的与性相关的恶性肿瘤，死亡率较高。前列腺特异性膜抗原（PSMA）在大多数前列腺肿瘤细胞表面过度表达，被认为是前列腺癌诊断和治疗的有价值的靶点。在过去十年中，基于 PSMA 配体的一系列放射性标记试剂已经被开发出来，并在原发性和复发性 PCa 的临床研究中显示出了有前景的结果。此外，镥-177-PSMA-617（177Lu-PSMA-617）放射治疗的鼓舞人心的反应和安全性为转移性去势抵抗性 PCa 提供了扩大治疗选择的潜力。回顾性队列研究表明，放射性标记的 PSMA 试剂是当前成功的主要手段，特别是在检测转移性和生化复发的前列腺癌方面。
本综述旨在全面介绍目前基于 PSMA 配体的放射性核素成像和治疗方法的文献，重点介绍那些已被临床采用的方法。
基于 PSMA 的诊断和治疗为改善前列腺癌的临床管理带来了很大的希望。
