Nawar Mohamed F, Selim Adli A, Essa Basma M, El-Daoushy Alaa F, Swidan Mohamed M, Chambers Claudia G, Al Qahtani Mohammed H, Smith Charles J, Sakr Tamer M
Department of Chemistry, Biochemistry and Pharmaceutical Sciences (DCBP), Faculty of Science, University of Bern, CH-3012 Bern, Switzerland.
Radioactive Isotopes and Generator Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo P.O. Box 13759, Egypt.
Cancers (Basel). 2025 Sep 18;17(18):3055. doi: 10.3390/cancers17183055.
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 [Ac]Ac/[Bi]Bi followed by the formulation of [Ac]Ac/[Bi]Bi-radiopharmaceuticals using different radiolabeling techniques. Finally, we have summarized the preclinical and clinical evaluation of these potential radiotheranostic agents.
α疗法（TAT）依靠将发射α粒子的放射性核素与特定的细胞靶向载体相结合，以传递高剂量的具有细胞毒性的辐射，从而能够破坏肿瘤组织。TAT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传递（LET）以及α粒子在组织中的短射程。最近的研究致力于在临床前和临床规模上评估TAT，包括评估对肿瘤组织的损伤以及对周围健康组织的毒性辐射影响最小。本综述强调了锕-225/铋-213放射性核素作为TAT有前景的候选物的应用。在此，我们首先讨论[Ac]Ac/[Bi]Bi的生产和供应，接着讨论使用不同放射性标记技术制备[Ac]Ac/[Bi]Bi放射性药物。最后，我们总结了这些潜在放射诊疗剂的临床前和临床评估。
