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

The approval of ²²³Ra dichloride (²²³RaCl₂) 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 ²²³RaCl₂ 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 ²²⁵Ac, ²¹³Bi, ²¹¹At, ²²⁷Th, and ²¹²Pb. Investigations incorporating ²²⁵Ac 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.