Potent candidates for Targeted Alpha Therapy (TAT)

IF 3.6 4区医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING

Nuclear medicine and biology Pub Date : 2025-05-13 DOI:10.1016/j.nucmedbio.2025.109027

Dmitry Filosofov , Ayagoz Baimukhanova , Jurabek Khushvaktov , Elena Kurakina , Valery Radchenko

引用次数: 0

Abstract

Targeted Alpha Therapy (TAT) holds significant promise as a localized treatment for cancer. Encouraging clinical results from using peptides and antibodies labeled with alpha emitters to treat patients with metastatic cancers, particularly those who have not responded to other therapies, provide compelling evidence of TAT's potential. To fully realize the benefits of TAT, it is essential to carefully select appropriate radionuclides and targeting delivery systems to maximize therapeutic efficacy while minimizing nonspecific toxicity to healthy tissues. This review explores key radiochemical, radiopharmaceutical, and radiation-biological considerations for current TAT candidates, and proposes additional potential candidates, establishing a foundation and criteria for the ongoing development of TAT radiopharmaceuticals.

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靶向α治疗（TAT）的有效候选药物

靶向α疗法（TAT）作为一种局部治疗癌症的方法具有重要的前景。使用带有α发射器标记的肽和抗体治疗转移性癌症患者，特别是那些对其他疗法没有反应的患者，令人鼓舞的临床结果为TAT的潜力提供了令人信服的证据。为了充分实现TAT的益处，必须仔细选择合适的放射性核素和靶向递送系统，以最大限度地提高治疗效果，同时最大限度地减少对健康组织的非特异性毒性。本综述探讨了当前TAT候选药物的关键放射化学、放射药物和辐射生物学考虑因素，并提出了其他潜在候选药物，为TAT放射性药物的持续开发奠定了基础和标准。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Nuclear medicine and biology 医学-核医学

CiteScore

6.00

自引率

9.70%

发文量

479

审稿时长

51 days

期刊介绍： Nuclear Medicine and Biology publishes original research addressing all aspects of radiopharmaceutical science: synthesis, in vitro and ex vivo studies, in vivo biodistribution by dissection or imaging, radiopharmacology, radiopharmacy, and translational clinical studies of new targeted radiotracers. The importance of the target to an unmet clinical need should be the first consideration. If the synthesis of a new radiopharmaceutical is submitted without in vitro or in vivo data, then the uniqueness of the chemistry must be emphasized. These multidisciplinary studies should validate the mechanism of localization whether the probe is based on binding to a receptor, enzyme, tumor antigen, or another well-defined target. The studies should be aimed at evaluating how the chemical and radiopharmaceutical properties affect pharmacokinetics, pharmacodynamics, or therapeutic efficacy. Ideally, the study would address the sensitivity of the probe to changes in disease or treatment, although studies validating mechanism alone are acceptable. Radiopharmacy practice, addressing the issues of preparation, automation, quality control, dispensing, and regulations applicable to qualification and administration of radiopharmaceuticals to humans, is an important aspect of the developmental process, but only if the study has a significant impact on the field. Contributions on the subject of therapeutic radiopharmaceuticals also are appropriate provided that the specificity of labeled compound localization and therapeutic effect have been addressed.