Hellwig D, Moosbauer J, Eilles C
Klinik für Nuklearmedizin, Universitätsklinikum des Saarlandes, Homburg.
Abteilung Nuklearmedizin, Universitätsklinikum Regensburg.
Aktuelle Urol. 2014 Nov;45(6):457-63. doi: 10.1055/s-0034-1395529. Epub 2014 Dec 17.
Prostate-specific membrane antigen (PSMA) is expressed as a cell surface protein physiologically in the prostate and can be found in all stages of prostate cancer. Even in castration-resistant prostate cancers, this overexpression of PSMA occurs. Due to the enzymatic activity of PSMA it was possible develop specific inhibitors from which "small molecule" radiopharmaceuticals were derived. By coupling the specific binding motif glutamate-urea-lysine with the chelator HBED-CC, which complexes Ga-68 very effectively, a new radiopharmaceutical is available for Ga-68-PSMA-PET/CT. According to the first results in patients with prostate carcinoma, this new diagnostic tool exhibited advantages in image quality compared to choline-PET/CT. An initial study demonstrated the higher contrast of the PET signal and an improved diagnostic accuracy. The properties of even further new PSMA PET radiopharmaceuticals can be of increasing importance for the diagnostic work-up of prostate cancer in all stages. In conjunction with therapeutic PSMA radiopharmaceuticals, a new field of theragnostics is opened.
前列腺特异性膜抗原（PSMA）在前列腺中作为一种细胞表面蛋白生理性表达，且在前列腺癌的各个阶段均可发现。即使在去势抵抗性前列腺癌中，PSMA也会出现这种过表达。由于PSMA的酶活性，有可能开发出特定抑制剂，从中衍生出“小分子”放射性药物。通过将特异性结合基序谷氨酸 - 脲 - 赖氨酸与能非常有效地络合镓 - 68的螯合剂HBED - CC偶联，一种用于镓 - 68 - PSMA - PET/CT的新型放射性药物问世。根据前列腺癌患者的初步结果，与胆碱 - PET/CT相比，这种新型诊断工具在图像质量方面表现出优势。一项初步研究证明了PET信号具有更高的对比度以及诊断准确性有所提高。甚至更多新型PSMA PET放射性药物的特性对于各阶段前列腺癌的诊断检查可能会变得越来越重要。与治疗性PSMA放射性药物相结合，一个新的治疗诊断领域被开辟出来。
