Nicolas Guillaume P, Morgenstern Alfred, Schottelius Margret, Fani Melpomeni
University Hospital Basel, University of Basel, Switzerland.
Directorate for Nuclear Safety and Security, Germany.
J Nucl Med. 2018 Dec 20. doi: 10.2967/jnumed.118.213496.
Peptide Receptor Radionuclide Therapy (PRRT) is an established treatment for non-operable or metastatic neuroendocrine neoplasms that express highly and frequently somatostatin receptors. More generally, PRRT is an attractive therapy option for delivering cytotoxic radiation to tumor cells through specific binding of a radiolabeled peptide to a molecular target. The development of imaging companions gave rise to the concept of radiotheranostics, important for in vivo tumor detection, characterization, staging but also, and more importantly, for individual patient selection and treatment. The success of somatostatin receptor targeting paved the way for the clinical translation of other peptide-based radiopharmaceuticals targeting, e.g. the receptors Cholecystokinin 2, Gastrin Releasing Peptide (GRPR), Neurokinin-1 and C-X-C motif chemokine 4 (CXCR4). While historically the Auger emitter In and the high-energy β- emitter Y were used, the vast majority of PRRT are currently performed with the medium-energy β- emitter Lu, while α emitters are increasingly studied in various clinical applications.
肽受体放射性核素治疗(PRRT)是一种针对无法手术切除或转移性神经内分泌肿瘤的既定治疗方法,这些肿瘤高度且频繁地表达生长抑素受体。更一般地说,PRRT是一种有吸引力的治疗选择,可通过放射性标记的肽与分子靶点的特异性结合,将细胞毒性辐射传递给肿瘤细胞。成像伴侣的发展催生了放射治疗诊断学的概念,这对于体内肿瘤检测、特征描述、分期很重要,但更重要的是,对于个体患者的选择和治疗也很重要。生长抑素受体靶向治疗的成功为其他基于肽的放射性药物靶向治疗的临床转化铺平了道路,例如靶向胆囊收缩素2、胃泌素释放肽(GRPR)、神经激肽-1和C-X-C基序趋化因子4(CXCR4)的受体。虽然历史上曾使用俄歇发射体铟和高能β发射体钇,但目前绝大多数PRRT是使用中能β发射体镥进行的,而α发射体在各种临床应用中也越来越受到研究。