靶向前列腺特异膜抗原的放射性诊断药物的研究现状和进展北大核心CSCD

前列腺癌是男性常见的恶性肿瘤之一,较高的发病率和死亡率使其成为男性健康的重大威胁。目前,前列腺癌的常见诊断方法无法对前列腺癌进行早期、准确的诊断,而正电子发射断层显像/计算机断层成像(PET/CT)及单光子发射计算机断层成像/计算机断层成像(SPECT/CT)可对前列腺癌的发生和发展进行有效地早期诊断。前列腺特异性膜抗原(prostate-specific membrane antigen,PSMA)在前列腺癌细胞表面高表达,是前列腺癌显像和治疗的较理想靶点。本文首先简介了前列腺癌的发病情况及现行常见的诊断方法,然后描述了PSMA的基本结构及与单克隆抗体和小分子抑制剂的作用机理,接着,重点叙述了基于PSMA的放射性诊断药物(主要是^(99)Tc^(m)、^(68)Ga和^(18)F标记的药物)的研究现状和进展,最后,还对PSMA放射性诊断药物的前景进行了展望。

Current Status and Progress of Diagnostic Radiopharmaceuticals Targeting Prostate-Specific Membrane Antigen

Prostate cancer is one of the most common cancers. High morbidity and mortality make it a significant threat to men’s health. Nowadays, standard diagnostic technologies could not provide effective and accurate imaging for early-stage prostate cancer. PET/CT and SPECT/CT could be used for early diagnosis of prostate cancer. Prostate-specific membrane antigen(PSMA) is widely overexpressed on the surface of prostate cancer cells, and it is an ideal target for the imaging and therapy of prostate cancer. This review first introduces the incidence of prostate cancer and current standard diagnostic methods and then describes the basic structure of PSMA and the interaction mechanism between PSMA and antibody or small molecule inhibitors. Next, it focuses on the research status and progress of diagnostic radiopharmaceuticals based on PSMA, especially emphasizing on ⁹⁹Tc^m, ⁶⁸Ga and ¹⁸F radiopharmaceuticals. In the end, the trend of PSMA targeting diagnostic radiopharmaceuticals is discussed.