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前列腺癌(prostate cancer,PCa)是男性泌尿生殖系统最常见的恶性肿瘤,严重危害中老年男性健康.前列腺特异性膜抗原(prostate specific membrane antigen,PSMA)是一种Ⅱ型跨膜糖蛋白,是PCa特异性分子靶点,于PCa发生进展、转移及去势抵抗性PCa(castration-resistant prostate cancer,CRPC)中高表达.PSMA特殊的理化结构及蛋白水解酶活性有利于靶向显像剂及抗肿瘤药物的开发.随着核医学仪器及分子探针研发新的进展,靶向PSMA的PET-CT/MRI分子探针在PCa的诊断、分期、再分期、生化复发探测及治疗决策中发挥着重要作用.本文紧跟国际研究热点,围绕PSMA靶向分子探针在核医学显像诊断及CRPC治疗中的最新进展综述如下.“,”Prostate cancer (PCa) is the most common malignant tumor in male genitourinary system,leading to substantial morbidity and mortality of the elderly.Prostate specific membrane antigen (PSMA) is a type Ⅱ transmembrane glycoprotein,which is a specific molecular target for PCa and expressed in most PCa patients.The special chemical constitution and enzyme activities of PSMA contribute to the development of highly selective antitumor drugs and targeting agents.Its expression levels are further enhanced in high grade,metastatic and castration resistant prostate cancer (CRPC).With the rapid developments of molecular probes and instruments in recent years,PSMA-targeted positron emission tomography-computer tomography/magnetic resonance imaging (PETCT/MRI) plays an important role in the diagnosis,staging,restaging,recurrence monitoring and therapeutic strategy of PCa.This review focuses on the latest progresses on PSMA based probe and theranostics in CRPC,which will contribute to the wide spreading of PSMA based theranostics in China.