Department of Nuclear Medicine, Postgraduate Institute of Medical Education and Research, Chandigarh.
Advanced Centre for Treatment, Research, and Education in Cancer, Navi Mumbai, Maharashtra, India.
Nucl Med Commun. 2022 Sep 1;43(9):970-977. doi: 10.1097/MNM.0000000000001594. Epub 2022 Jun 23.
Actinium-225 (225Ac) has emerged as a promising therapeutic radioisotope for targeted alpha therapy. It emits net four alpha particles during its decay to stable daughter bismuth-209, rightly called an in-vivo nano-generator. Compared to the worldwide demand of 225Ac, the amount produced via depleted thorium-229 sources is minimal, making it an expensive radionuclide. However, many research groups are working on optimizing the parameters for the production of 225Ac via different routes, including cyclotrons, reactors and high-energy linear accelerators. The present review article focuses on the various aspects associated with the development of 225Ac radiopharmaceuticals. It includes the challenges and opportunities associated with the production methods, labeling chemistry, in-vivo kinetics and dosimetry of 225Ac radiopharmaceuticals. A brief description is also given about the 225Ac radiopharmaceuticals at preclinical stages, clinical trials and used routinely.
锕-225（225Ac）已成为靶向α治疗有前途的治疗放射性同位素。它在衰变为稳定的子体铋-209 的过程中发射四个净α粒子，因此被恰当地称为体内纳米发生器。与全球对 225Ac 的需求相比，通过贫化钍-229 源生产的数量微不足道，这使其成为一种昂贵的放射性核素。然而，许多研究小组正在通过不同的途径（包括回旋加速器、反应堆和高能直线加速器）优化 225Ac 的生产参数。本文综述了与 225Ac 放射性药物开发相关的各个方面。它包括与生产方法、标记化学、体内动力学和 225Ac 放射性药物的剂量学相关的挑战和机遇。还简要描述了处于临床前阶段、临床试验阶段和常规使用的 225Ac 放射性药物。
