Cationic radionuclides and ligands for targeted therapeutic radiopharmaceuticals

This review considers the already used and potential alpha- and beta-emitting cationic radionuclides for targeted radionuclide therapy. Recent results of laboratory, preclinical and clinical applications of these radionuclides are discussed. As opposed to beta-emitters, which are already used in nuclear medicine, alpha-emitters involved in targeted radiopharmaceuticals were subjected to clinical trials only recently and were found to be therapeutically effective. The review summarizes recent trends in the development of ligands as components of radiopharmaceuticals addressing specific features of short-lived cationic radionuclides applied in medicine. Despite a steadily growing number of chelating ligands, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and diethylenetriaminepentaacetic acid (DTPA) remain the most widely used agents in nuclear medicine. The drawbacks of these compounds restrict the application of radionuclides in medicine. Variations in the macrocycle size, the introduction and modification of substituents can significantly improve the chelating ability of ligands, enhance stability of radionuclide complexes with these ligands and eliminate the influence of ligands on the affinity of biological targeting vectors.