α放射性金属药物的研究现状与展望

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²²⁵Ac、^212/213Bi、²¹²Pb、²²⁷Th以及²²³Ra。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。

Alpha-Emitting Metallic Radiopharmaceuticals:Current Status and Future Prospects

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 to β-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 ²²⁵Ac, ^212/213Bi, ²¹²Pb, ²²⁷Th and ²²³Ra. Firstly, the physical, radiobiological properties of α-particle and β-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.