Targeted α-Therapy in Cancer Management: Synopsis of Preclinical and Clinical Studies

The approval of 223 Ra dichloride ( 223 RaCl 2 ) in 2013 was a principal event in introducing targeted α-therapy as a form of safe and effective management strategy in cancer. There is an increasing interest in research and development of new targeted α-therapy agents spearheaded by advancements in cancer biology, radiochemistry, and availability of clinically relevant α particles. There are active clinical studies on sequencing or combining 223 RaCl 2 with other drug regimens in the setting of metastatic prostate cancer and in other cancers such as osteosarcoma and bone-dominant breast cancer. Targeted α-therapy strategy is also being actively explored through many preclinical and few early clinical studies using 225 Ac, 213 Bi, 211 At, 227 Th, and 212 Pb. Investigations incorporating 225 Ac are more robust and active at this time with promising results. The author provide a brief synopsis of the preclinical and clinical studies in the rapidly evolving field of targeted α-therapy in cancer management.