摘要
神经内分泌瘤(NET)是起源于神经内分泌细胞的肿瘤,可发生在体内各处,最常见在胃、肠、胰腺等消化系统中。近年来,放射性药物利用核素衰变特性应用于恶性肿瘤诊断与治疗的潜力被充分开发,成为实现精准医疗的新手段。大多数NET细胞的表面过表达生长抑素受体(SSTR),为放射性药物实现特异性靶向提供了机会。177Lu-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸-D-苯丙氨酸1-酪氨酸3-苏氨酸8-奥曲肽(177Lu-DOTA-TATE)是一种肽受体介导的放射性核素治疗药物,可与肿瘤细胞膜上的SSTR特异性结合,进而对SSTR阳性的胃肠胰NET进行治疗。笔者对177Lu-DOTA-TATE的药物基本信息、研发历程、作用机制及临床应用进展进行了综述,为未来肽受体放射性核素治疗药物的研发及药物联合治疗的开展提供参考。
Neuroendocrine tumors(NET)are originated from neuroendocrine cells,which can occur in various parts of the body,most commonly in the digestive system,such as the stomach,intestines and pancreas.In recent years,the potential of radiopharmaceuticals to be applied to the diagnosis and treatment of malignant tumors using the decay properties of nuclides has been fully exploited,and has become a new means to achieve precision medical treatment.Since most NET cells overexpress somatostain receptors(SSTR)on their surface,it provides an opportunity for radiopharmaceuticals to achieve specific targeting.177Lu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-D-Phe1-Tyr3-Thr8-octreotide(177Lu-DOTA-TATE),a peptide receptor-mediated radionuclide therapeutic drug,can bind specifically to SSTR on the membrane of tumour cells,thereby treating SSTR-positive gastroenteropancreatic NET.The authors reviewed the drug basic information,research and development process,mechanism of action,and clinical application progress of 177Lu-DOTA-TATE,to serve as a reference for the development of peptide receptor radionuclide therapy drug and the implementation of clinical combination treatment in the future.
作者
杨双萌
于江
侯文彬
李祎亮
Yang Shuangmeng;Yu Jiang;Hou Wenbin;Li Yiliang(The Graduate School of Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;State Key Laboratory of Advanced Medical Materials and Devices,Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine,Tianjin Institute of Health Science,Institute of Radiation Medicine,Chinese Academy of Medical Science,Peking Union Medical College,Tianjin 300192,China)
出处
《国际放射医学核医学杂志》
2025年第7期456-462,共7页
International Journal of Radiation Medicine and Nuclear Medicine
基金
中国医学科学院医学与健康科技创新工程国家医学健康科技战略平台与体系建设专项(2022-I2M-2-003)。
关键词
镥
奥曲肽
神经内分泌瘤
受体
生长抑素
肽受体放射性核素治疗
Lutetium
Octreotide
Neuroendocrine tumors
Receptors,somatostatin
Peptide receptor radionuclide therapy
