α放射性金属药物的研究现状与展望  

Alpha-Emitting Metallic Radiopharmaceuticals:Current Status and Future Prospects

作　　者：崔海平 沈浪涛 CUI Hai-ping;SHEN Lang-tao(HTA Co.Ltd,Beijing 102413,China;Innovation Center of Radiopharmaceutical,China Isotope&Radiation Corporation,Beijing 102413,China;National Isotope Center of Engineering and Technology,China Institute of Atomic Energy,Beijing 102413,China)

机构地区：[1]原子高科股份有限公司,北京102413 [2]中国同辐放药研发中心,北京102413 [3]中国原子能科学研究院国家同位素工程技术研究中心,北京102413

出　　处：《核化学与放射化学》2020年第6期524-538,共15页Journal of Nuclear and Radiochemistry

摘　　要：靶向α治疗(TAT)是一种很有前景的肿瘤治疗方法。在TAT中,把含有α发射体核素的放射性药物的辐射选择性地传送到癌症细胞,而尽可能将全身的毒副作用最小化。与β粒子相比,α粒子具有更高的能量、更高的线性能量传递(LET)和更短的组织穿透距离。因此,TAT在靶向治疗中具有明显的优势。本文概述了用于TAT的一些锕系元素和它们的放射性金属衰变子体。这些放射性金属核素包括225 Ac、212/213 Bi、212 Pb、227 Th以及223 Ra。首先比较了α粒子和β粒子的物理和辐射生物学性质。然后,描述了这些放射性金属核素的化学性质和来源。接着,展示了TAT中常用的一些双功能螯合剂。其后,介绍了TAT放射性药物的研究现状。最后,给出了TAT放射性药物研发中的挑战性问题和前景展望。Targeted alpha therapy(TAT)is a very promising therapeutic way for the treatment of cancers.In TAT,a radiopharmaceutical containing alpha-emitter radionuclide was used to deliver systemic radiation selectively to cancer cell while minimizing systemic toxic effects.In comparison toβ-particle,α-particle has higher energy,higher linear energy transfer(LET)and a shorter penetration range in tissues.Therefore,TAT has distinct advantages for use in targeted therapy.In this review,some actinoid elements and the radiometallic decay daughters of these actinoid elements,used in TAT,were discussed.These radiometallic nuclides included 225 Ac,212/213 Bi,212 Pb,227 Th and 223 Ra.Firstly,the physical,radiobiological properties ofα-particle andβ-particle were compared.Secondly,the chemical properties and their source of these radiometallic nuclides were described.Thirdly,the selected bifunctional chelators of TAT radiopharmaceuticals were presented.Fourthly,the current status of TAT radiopharmaceuticals was introduced.Lastly,our views about the future challenges and prospects of TAT radiopharmaceuticals were given.

关 键 词：靶向α治疗 放射性药物 锕系元素 ^225 Ac ^212/213 Bi ^212 Pb ^227 Th ^223 Ra 

分 类 号：R817.8[医药卫生—影像医学与核医学]