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使用铋-213和锕-225的靶向α疗法:满足未来需求。

Targeted alpha therapy with bismuth-213 and actinium-225: Meeting future demand.

作者信息

Bruchertseifer Frank, Kellerbauer Alban, Malmbeck Rikard, Morgenstern Alfred

机构信息

European Commission, Joint Research Centre (JRC), Karlsruhe, Germany.

出版信息

J Labelled Comp Radiopharm. 2019 Sep;62(11):794-802. doi: 10.1002/jlcr.3792. Epub 2019 Aug 1.

DOI:10.1002/jlcr.3792
PMID:31369165
Abstract

Targeted alpha therapy (TAT) is a promising approach for the treatment of cancer. The use of alpha emitters for cancer therapy has two distinct advantages over conventional therapies. The short range of alpha radiation in human tissue (less than 0.1 mm), corresponding to only a few cell diameters, allows selective killing of targeted cancer cells while sparing surrounding healthy tissue. At the same time, the high energy (several MeV) of alpha radiation and its associated high linear energy transfer leads to highly effective cell kill. Consequently, alpha radiation can destroy cells which otherwise exhibit resistance to treatment with beta or gamma irradiation or chemotherapeutic drugs, and can thus offer a therapeutic option for tumors resistant to conventional therapies. Recent results demonstrating the remarkable therapeutic efficacy of alpha emitters to treat various cancers have underlined the clinical potential of TAT. This paper describes the recent clinical experience with Bi and Ac. In view of the enormous benefit of targeted cancer treatment with alpha emitters, their production will have to be considerably increased beyond current supply capabilities. Alternative production methods based on the irradiation of uranium, thorium, or radium targets at reactors or accelerator facilities have the potential to meet future demand.

摘要

靶向α治疗(TAT)是一种很有前景的癌症治疗方法。与传统疗法相比,使用α发射体进行癌症治疗有两个明显的优势。α辐射在人体组织中的射程较短(小于0.1毫米),仅相当于几个细胞直径,这使得在不损伤周围健康组织的情况下能够选择性地杀死靶向癌细胞。同时,α辐射的高能量(几兆电子伏特)及其相关的高线性能量传递导致细胞杀伤效率很高。因此,α辐射能够破坏那些对β或γ辐射或化疗药物治疗具有抗性的细胞,从而为对传统疗法耐药的肿瘤提供一种治疗选择。最近的结果表明α发射体在治疗各种癌症方面具有显著的治疗效果,这突出了TAT的临床潜力。本文描述了使用铋和锕的近期临床经验。鉴于使用α发射体进行靶向癌症治疗的巨大益处,其产量必须大幅增加,远远超出目前的供应能力。基于在反应堆或加速器设施中对铀、钍或镭靶进行辐照的替代生产方法有潜力满足未来的需求。

相似文献

1
Targeted alpha therapy with bismuth-213 and actinium-225: Meeting future demand.使用铋-213和锕-225的靶向α疗法:满足未来需求。
J Labelled Comp Radiopharm. 2019 Sep;62(11):794-802. doi: 10.1002/jlcr.3792. Epub 2019 Aug 1.
2
An Overview of Targeted Alpha Therapy with Actinium and Bismuth.锕和铋靶向α治疗概述
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The Evolving Clinical Role of Actinium-225 and Bismuth-213 for Targeted Alpha Therapy (TAT) - Production, Radiopharmaceutical Development and Clinical Applications.锕-225和铋-213在靶向α治疗(TAT)中的临床作用演变——生产、放射性药物研发及临床应用
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Molecules. 2018 Mar 5;23(3):581. doi: 10.3390/molecules23030581.
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Bismuth-213 and actinium-225 -- generator performance and evolving therapeutic applications of two generator-derived alpha-emitting radioisotopes.铋 - 213和锕 - 225——两种基于发生器产生的α发射性放射性同位素的发生器性能及不断发展的治疗应用
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Supply and Clinical Application of Actinium-225 and Bismuth-213.锕-225 和铋-213 的供应和临床应用。
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Development of Targeted Alpha Therapy from Bench to Bedside.靶向α治疗从实验室到临床的发展
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Alpha emitting nuclides for targeted therapy.用于靶向治疗的发射阿尔法粒子的核素。
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引用本文的文献

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Sci Rep. 2025 Jul 2;15(1):23563. doi: 10.1038/s41598-025-02277-4.
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Production and purification of molecular Ac at CERN-ISOLDE.欧洲核子研究中心-同位素分离器在线装置(CERN-ISOLDE)中分子Ac的生产与纯化。
J Radioanal Nucl Chem. 2025;334(1):367-379. doi: 10.1007/s10967-024-09811-0. Epub 2024 Nov 15.
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Actinium chelation and crystallization in a macromolecular scaffold.
在大分子支架中锕的螯合和结晶。
Nat Commun. 2024 Jul 15;15(1):5741. doi: 10.1038/s41467-024-50017-5.
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Phage-encoded bismuth bicycles enable instant access to targeted bioactive peptides.噬菌体编码的铋双环化合物可实现对靶向生物活性肽的快速获取。
Commun Chem. 2024 Jun 27;7(1):143. doi: 10.1038/s42004-024-01232-0.
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Targeted Alpha Therapy: All We Need to Know about Ac's Physical Characteristics and Production as a Potential Theranostic Radionuclide.靶向α治疗:关于作为一种潜在的治疗诊断放射性核素的锕的物理特性及生产我们需要了解的一切。
Pharmaceuticals (Basel). 2023 Dec 2;16(12):1679. doi: 10.3390/ph16121679.
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Radiometals in Imaging and Therapy: Highlighting Two Decades of Research.成像与治疗中的放射性金属:二十年来的研究亮点。
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Investigation of the Effect on the Albumin Binding Moiety for the Pharmacokinetic Properties of Ga-, Bi-, and Lu-Labeled NAPamide-Based Radiopharmaceuticals.镓、铋和镥标记的基于NAP酰胺的放射性药物的白蛋白结合部分对药代动力学性质的影响研究。
Pharmaceuticals (Basel). 2023 Sep 11;16(9):1280. doi: 10.3390/ph16091280.
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Resonant laser ionization and mass separation of Ac.锕系元素的共振激光电离和质量分离
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