α核素225Ac的制备及医学应用现状

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。

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

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.