文章：

锕-225/铋-213作为靶向α疗法的潜在主导核素：当前供应现状、应用障碍与未来展望

Actinium-225/Bismuth-213 as Potential Leaders for Targeted Alpha Therapy: Current Supply, Application Barriers, and Future Prospects

原文发布日期：18 September 2025

DOI: 10.3390/cancers17183055

类型: Article

开放获取: 是

英文摘要：

Alpha therapy (TAT) relies on combining alpha-emitting radionuclides with specific cell-targeting vectors to deliver a high payload of cytotoxic radiation capable of destroying tumor tissues. TAT efficacy comes from the tissue selectivity of the targeting vector, the high linear energy transfer (LET) of the radionuclide, and the short range of alpha particles in tissues. Recent research studies have been directed to evaluate TAT on a preclinical and clinical scale, including evaluating damage to tumor tissues with minimal toxic radiation effects on surrounding healthy tissues. This review highlights the use of Actinium-225/Bismuth-213 radionuclides as promising candidates for TAT. Herein, we begin with a discussion on the production and supply of [225Ac]Ac/[213Bi]Bi followed by the formulation of [225Ac]Ac/[213Bi]Bi-radiopharmaceuticals using different radiolabeling techniques. Finally, we have summarized the preclinical and clinical evaluation of these potential radiotheranostic agents.

摘要翻译： 

α粒子治疗（TAT）通过将α发射放射性核素与特异性细胞靶向载体相结合，实现高剂量细胞毒性辐射的精准递送，从而有效摧毁肿瘤组织。该疗法的疗效源于靶向载体的组织选择性、放射性核素的高线性能量转移（LET）特性以及α粒子在组织中的短射程优势。近期研究聚焦于TAT的临床前及临床评估，重点考察其对肿瘤组织的杀伤效果，同时最大限度降低对周围健康组织的辐射毒性。本综述重点探讨锕-225/铋-213放射性核素作为TAT候选药物的应用前景：首先系统阐述[225Ac]Ac/[213Bi]Bi的生产与供应体系，继而详述采用不同放射性标记技术制备[225Ac]Ac/[213Bi]Bi放射性药物的工艺路径，最后全面总结这些潜在放射性诊疗药物的临床前及临床评估进展。

原文链接：

Actinium-225/Bismuth-213 as Potential Leaders for Targeted Alpha Therapy: Current Supply, Application Barriers, and Future Prospects