同位素 ›› 2022, Vol. 35 ›› Issue (3): 179-188.DOI: 10.7538/tws.2022.35.03.0179

• 放射性治疗药物专辑 • 上一篇    下一篇

α核素225Ac的制备及医学应用现状

赵紫宇;温凯;马承伟;褚浩淼;段菲;李光;李忠勇   

  1. 原子高科股份有限公司,北京102413
  • 出版日期:2022-06-20 发布日期:2022-06-20

Research Status of Alpha-Emitting Radionuclide 225Ac: Preparation and Medical Application

ZHAO Ziyu;WEN Kai;MA Chengwei;CHU Haomiao;DUAN Fei;LI Guang;LI Zhongyong   

  1. HTA Co., Ltd., Beijing 102413, China
  • Online:2022-06-20 Published:2022-06-20

摘要: 靶向α治疗(targeted alpha therapy, TAT)是一种基于发射α粒子的放射性核素与肿瘤选择性载体分子作为特定靶向癌细胞载体的核医学治疗方式。由于对靶向癌细胞具有强杀伤力,而对非靶向正常组织的损伤小,TAT成为一种很有前景的肿瘤治疗方法。225Ac核素因其适宜的半衰期、独特的衰变性质、易于配位等特点,成为TAT中α核素的最佳选择之一。研究表明,225Ac的靶向药物结构在癌症治疗中有着优异的效果,但是225Ac核素的制备却仍处于研究阶段。本文对225Ac核素性质、制备工艺以及用于TAT的225Ac放射性药物现状进行了总结,并对225Ac的制备和药物标记进行了展望。预计在不久的将来,医用级225Ac将实现批量化生产,225Ac标记的放射性药物将有望获批用于肿瘤治疗。

关键词: TAT, 225Ac, 制备方法, 225Ac药物

Abstract: Targeted alpha therapy (TAT) is a kind of nuclear medicine treatment based on alpha-emitting radionuclides and tumor-selective carrier molecules for targeted cancer cells. Due to its strong toxicity to targeted cancer cells and relatively less toxic to normal tissues, TAT has been a promising tumor treatment method. Attributed to its suitable half-life (9.9 d), unique decay properties (decay produceing 4α+2β particles), and suitable coordination, 225Ac has become one of the best choice for α nuclides in TAT. Studies have shown that the targeted 225Ac-radiopharmaceuticals exhibit excellent effectiveness on cancer treatment, but the preparation of 225Ac is facing research difficulties. This article summarized the properties of 225Ac nuclide, the status of the preparation process and 225Ac-radiopharmaceuticals for TAT. And prospects were proposed for the production process of 225Ac and its medical application. It is expected that the large-scale production of medical 225Ac will be standardized, and 225Ac-radiopharmaceuticals will be approved for tumor treatment in the future.

Key words: TAT, 225Ac, production method, 225Ac radiopharmaceuticals