Journal of Isotopes ›› 2020, Vol. 33 ›› Issue (4): 241-249.DOI: 10.7538/tws.2019.youxian.017

Previous Articles     Next Articles

Research Progress of Radionuclide-Labeled PSMA Ligands in the Diagnosis and Treatment of Prostate Cancer

LIU Jingru;ZHU Hong   

  1. Jinling Hospital Department of Nuclear Medicine, Nanjing University School of Medicine, Nanjing 210002, China
  • Online:2020-08-20 Published:2020-09-12



  1. 东部战区总医院(原南京军区南京总医院) 核医学科,江苏 南京210002


Prostate cancer (PCa) is a malignant solid tumor with a high incidence in middle-aged and elderly men. At present, the diagnosis and treatment of PCa is limited and the sensitivity of the diagnostic method is not high, which is extremely unfavorable for the early diagnosis and late detection of PCa patients. Prostate-specific membrane antigen (PSMA) is a type Ⅱ glutamate carboxypeptidase that is overexpressed on the surface of almost all PCa cells, and the degree of overexpression of PSMA increases with the progression, metastasis and recurrence of PCa, Therefore, PSMA can be used as a specific target for the diagnosis and treatment of PCa. In recent years, with the development of nuclear medicine instruments and radioactive molecular probes, some PET/CT and SPECT/CT molecular probes targeting PSMA, such as 111In-capromab, 18F-DCFPyL, 99mTc-MIP-1405, 131I-MIP-1095, 68Ga-PSMA-11 and 177Lu-PSMA-617 have received extensive attention and application in the diagnosis, staging, biochemical recurrence detection and treatment of PCa. In this review, the latest research progress of PSMA ligands is summarized from the aspects of ligand affinity, selectivity, structure-activity relationship, in vivo metabolism and clinical application, which is expected to be beneficial to the research and development of new generation of PSMA inhibitors.

Key words: prostate cancer, PSMA, PSMA ligands, radionuclide imaging



关键词: 前列腺癌, 前列腺特异性膜抗原, PSMA配体, 放射性核素显像