Astatine-211 Radiopharmaceuticals; Status, Trends, and the Future

Abstract: The low range of alpha particles provides an opportunity to better target cancer cells theoretically leading to the introduction of interesting alpha emitter radiopharmaceuticals including 225Ac, 212Pb, etc. The combination of high energy and short range of alpha emitters differentiates targeted radiotherapy from other methods and reduces unwanted cytotoxicity of the cells around the tumoral tissue. Among interesting alpha emitters candidates for targeted therapy, 211At, one of the radioisotopes with the best optimal decay properties, shows great promise for targeted radiotherapy in some animal prostate cancer xenograft studies and bone micro tumors with significant effects compared to other beta and alpha emitters and also demonstrates interesting properties for clinical applications. However, production and application of this alpha emitter in the development of actinium-based radiopharmaceuticals is hampered by many obstacles. This mini-review demonstrates 211At production methods, chemical separation, radiolabeling procedures, 211At-radiopharmaceuticals and their clinical trials, transport, logistics, and costs and future trends in the field for ultimate clinical applications. This review showed that there are limited clinical trials on 211Ac-based radiopharmaceuticals, which is due to the low accessibility of this radioisotope and other limitations. However, the development programs of major industries indicate the development of 211Ac-based radiopharmaceuticals in the future.