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²²⁵Ac is one of the most promising radionuclides in alpha particle targeting therapy (targeted alpha therapy, TAT). The alpha particles produced by ²²⁵Ac decay have the characteristics of higher linear energy transfer, shorter tissue action distance, less side effects and so on. Therefore, TAT drugs such as small molecules and antibodies labeled with ²²⁵Ac have good application prospects in tumor treatment. This paper introduces the decay properties and sources of ²²⁵Ac, summarizes the commonly used chelating agents for ²²⁵Ac labeling, exemplifies the process of ²²⁵Ac labeling, and summarizes the application of ²²⁵Ac-labeled compounds in non-clinical and clinical research in the past three years. Finally, the challenges and prospects of ²²⁵Ac-labeled TAT drugs are analyzed, which provides a basis for the follow-up development of TAT drugs.

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²²⁵Ac是α粒子靶向治疗（targeted alpha therapy, TAT）中最有前景的放射性核素之一，²²⁵Ac衰变产生的α粒子具有较高的线性能量传递、较短的组织作用距离、较小的不良反应等特性。因此，通过²²⁵Ac标记的小分子、抗体等TAT药物在肿瘤治疗中具有良好的应用前景，本文介绍了²²⁵Ac的衰变性质与来源，概述了²²⁵Ac标记常用的螯合剂，举例说明了²²⁵Ac标记的过程，总结了近3年²²⁵Ac标记的化合物在非临床与临床研究中的应用，最后分析了²²⁵Ac标记的TAT药物面临的挑战与前景，为后续TAT药物研发提供基础。

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宋鑫，女，硕士研究生，主要从事药动学研究。E-mail: xsong.hm@simm.ac.cn。

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宋鑫，女，硕士研究生，主要从事药动学研究。E-mail: xsong.hm@simm.ac.cn。

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