基于生长抑素受体靶向的放射性金属药物的研究进展  被引量:1

Research Progress of Metal-Based Radiopharmaceuticals Targeting Somatostatin Receptor

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作  者:秦祥宇 沈浪涛 QIN Xiang-yu;SHEN Lang-tao(China Atomic Energy Authority Center of Excellence on Nuclear Technology Applications for Engineering and Industrialization of Radiopharmaceuticals,China National Nuclear Corporation Engineering Research Center of Radiopharmaceuticals,HTA Co.Ltd,Beijing 102413,China)

机构地区:[1]国家原子能机构核技术(放射性药物工程转化)研发中心,中国核工业集团有限公司放射性药物工程技术研究中心,原子高科股份有限公司,北京102413

出  处:《核化学与放射化学》2023年第2期119-132,I0003,共15页Journal of Nuclear and Radiochemistry

基  金:“十三五”核能开发基金项目;中核集团青年英才计划资助项目。

摘  要:神经内分泌肿瘤(neuroendocrine tumors,NETs)是一组起源于神经内分泌细胞的异质性肿瘤。它们可以发生在身体的任何部位,最常见于消化道、胰腺和肺。近年来NET的发病率和流行率均在逐年上升。NET的早期诊断一直很困难。生长抑素受体(somatostatin receptor,SSTR)作为NET中最常见的肽激素受体,已成为NET药物研发中的重要靶点。放射性核素标记的生长抑素类似物可与NET细胞表面过表达的SSTR特异性结合,因此,此类放射性药物可用于NET的早期诊断和靶向治疗。到目前为止,已有多个SSTR靶向放射性药物被美国食品药品监督管理局(FDA)、欧洲药监局(EMA)等机构批准上市,但在中国还没有此类上市的放射性药物。本文介绍了神经内分泌肿瘤与SSTR的关系以及生长抑素类放射性金属药物的研发历史,总结了已被FDA等各国药品监管部门批准的放射性诊断和治疗药物,然后介绍了生长抑素受体激动剂和拮抗剂药物的不同特点,评述了SSTR拮抗剂在放射性诊断和治疗领域的相关研究进展,基于SSTR拮抗剂的放射性金属药物已初步显示了比激动剂更好的诊断和治疗效果,可能具有良好的应用前景。Neuroendocrine tumors(NETs)are a group of heterogeneous tumors originating from neuroendocrine cells.They can occur anywhere in the body,most commonly in the digestive tract,pancreas,and lungs.The incidence and prevalence of NET have been increasing in recent years.Early diagnosis of NET has been difficult.Somatostatin receptor(SSTR),as the most common peptide hormone receptor in NET,has become an important target in NET drug development.Radionuclide-labeled somatostatin analogs can specifically bind to SSTR over-expressed on the surface of NET cells.Therefore,such radiopharmaceuticals can be used for early diagnosis and targeted therapy of NET.So far,several SSTR-targeted radiopharmaceuticals have been approved for marketing by the U.S.Food and Drug Administration(FDA),European Medicines Agency(EMA)and other agencies,but no such radiopharmaceuticals have been marketed in China.This review first introduces the relationship between neuroendocrine tumors and SSTR,and the development history of SSTR-targeted metal-based radiopharmaceuticals,and summarizes the diagnostic and therapeutic radiopharmaceuticals that have been approved by the FDA and other drug regulatory authorities in various countries.The different characteristics of SSTR antagonists and antagonist drugs are discussed,and the related research progress of SSTR antagonists in the field of radioactive diagnosis and therapy is remarked.Metal-based radiopharmaceuticals targeting SSTR antagonists have initially shown better diagnostic and therapeutic effects than agonists,and may have good application prospects.

关 键 词:生长抑素受体 神经内分泌肿瘤 拮抗剂 放射性金属药物 

分 类 号:R817[医药卫生—影像医学与核医学]

 

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