Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical School, Baltimore, MD 21287, USA.
Curr Top Med Chem. 2013;13(8):951-62. doi: 10.2174/1568026611313080008.
Prostate cancer (PCa) is the second leading cause of cancer-related death in American men. Positron emission tomography/computed tomography (PET/CT) with emerging radiopharmaceuticals promises accurate staging of primary disease, restaging of recurrent disease, detection of metastatic lesions and, ultimately, for predicting the aggressiveness of disease. Prostate-specific membrane antigen (PSMA) is a well-characterized imaging biomarker of PCa. Because PSMA levels are directly related to androgen independence, metastasis and progression, PSMA could prove an important target for the development of new radiopharmaceuticals for PET. Preclinical data for new PSMA-based radiotracers are discussed and include new (89)Zr- and (64)Cu-labeled anti-PSMA antibodies and antibody fragments, (64)Cu-labeled aptamers, and (11)C-, (18)F-, (68)Ga-, (64)Cu-, and (86)Y-labeled low molecular weight inhibitors of PSMA. Several of these agents, namely (68)Ga- HBED-CC conjugate 15, (18)F-DCFBC 8, and BAY1075553 are particularly promising, each having detected sites of PCa in initial clinical studies. These early clinical results suggest that PET/CT using PSMA-targeted agents, especially with compounds of low molecular weight, will make valuable contributions to the management of PCa.
前列腺癌（PCa）是美国男性癌症相关死亡的第二大主要原因。新兴放射性药物正电子发射断层扫描/计算机断层扫描（PET/CT）有望准确分期原发性疾病、复发性疾病分期、检测转移性病变，并最终预测疾病的侵袭性。前列腺特异性膜抗原（PSMA）是一种经过充分研究的 PCa 成像生物标志物。由于 PSMA 水平与雄激素非依赖性、转移和进展直接相关，因此 PSMA 可能成为开发用于 PET 的新型放射性药物的重要靶标。讨论了新型基于 PSMA 的放射性示踪剂的临床前数据，包括新型（89）Zr-和（64）Cu 标记的抗 PSMA 抗体和抗体片段、（64）Cu 标记的适体以及（11）C-、（18）F-、（68）Ga-、（64）Cu-和（86）Y-标记的 PSMA 低分子量抑制剂。其中几种药物，即（68）Ga-HBED-CC 缀合物 15、（18）F-DCFBC 8 和 BAY1075553 特别有前途，每种药物在最初的临床研究中都检测到了 PCa 部位。这些早期临床结果表明，使用 PSMA 靶向药物的 PET/CT，特别是使用低分子量化合物，将对 PCa 的治疗做出有价值的贡献。
