The Evolving Coordination Chemistry of Radiometals for Targeted Alpha Therapy

Several radiometals are of interest in the development of new alpha-emitting radiopharmaceuticals. This review highlights the role of coordination chemistry in the design of Ac-225, Bi-212/213, Pb-212, Tb-149, Th-227, and Ra-223/224 radiopharmaceuticals to treat cancer. Several chelators have recently been developed that are addressing the specific requirements of each radiometal to provide outstanding radiolabelling and in vivo properties. These advances are supporting the momentum that is building around radiopharmaceuticals for targeted alpha therapy.