神经内分泌肿瘤治疗药物177Lu-DOTA-TATE的研究进展

Research advances in 177Lu-DOTA-TATE for the treatment drugs of neuroendocrine neoplasms

  • 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。

     

    Abstract: 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.

     

/

返回文章
返回