Radiopharmaceuticals have become an increasingly important modality for both the diagnosis and treatment of numerous diseases, particularly cancer. Their active moiety is usually a radioactive metal ion, bound to a tumor targeting molecule via a chelating agent. Among the plethora of chelators developed for this purpose, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is undoubtedly one of the most widely employed. This review examines selected properties of metal-DOTA complexes that are relevant to radiopharmaceutical applications. The discussion focuses on elements that have radioisotopes of current, past, or potential future clinical relevance: actinium, antimony, barium, bismuth, cerium, cobalt, copper, erbium, gallium, gold, holmium, indium, iridium, lanthanum, lead, lutetium, manganese, mercury, niobium, osmium, palladium, platinum, radium, rhenium, rhodium, rubidium, ruthenium, samarium, scandium, silver, strontium, tantalum, technetium, terbium, thallium, thorium, titanium, uranium, yttrium, and zirconium. The properties considered include: (i) speciation in aqueous solution (number, stoichiometry, and stability constants of metal-DOTA complexes); (ii) structure of the complexes; and (iii) kinetics of complex formation and dissociation. These data have been collected in a "DOTA Periodic Table of Elements of Radiopharmaceutical Interest", which provides a compact graphical overview of the available information. In addition, the review summarizes radiochemical properties of metal-DOTA complexes, including radiolabeling yields and stability in biological environments. Despite the substantial body of literature on metal-DOTA complexes, this analysis reveals that important gap remains. For several elements, thermodynamics, structural or kinetic parameters are still unavailable, while in other cases reported data show significant variability and warrant critical re-evaluation.
One ring to bind them all? A review on speciation, structure, kinetics, and radiochemistry of DOTA complexes formed with medically relevant radiometals
Franchi S.;Di Marco V.
2026
Abstract
Radiopharmaceuticals have become an increasingly important modality for both the diagnosis and treatment of numerous diseases, particularly cancer. Their active moiety is usually a radioactive metal ion, bound to a tumor targeting molecule via a chelating agent. Among the plethora of chelators developed for this purpose, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is undoubtedly one of the most widely employed. This review examines selected properties of metal-DOTA complexes that are relevant to radiopharmaceutical applications. The discussion focuses on elements that have radioisotopes of current, past, or potential future clinical relevance: actinium, antimony, barium, bismuth, cerium, cobalt, copper, erbium, gallium, gold, holmium, indium, iridium, lanthanum, lead, lutetium, manganese, mercury, niobium, osmium, palladium, platinum, radium, rhenium, rhodium, rubidium, ruthenium, samarium, scandium, silver, strontium, tantalum, technetium, terbium, thallium, thorium, titanium, uranium, yttrium, and zirconium. The properties considered include: (i) speciation in aqueous solution (number, stoichiometry, and stability constants of metal-DOTA complexes); (ii) structure of the complexes; and (iii) kinetics of complex formation and dissociation. These data have been collected in a "DOTA Periodic Table of Elements of Radiopharmaceutical Interest", which provides a compact graphical overview of the available information. In addition, the review summarizes radiochemical properties of metal-DOTA complexes, including radiolabeling yields and stability in biological environments. Despite the substantial body of literature on metal-DOTA complexes, this analysis reveals that important gap remains. For several elements, thermodynamics, structural or kinetic parameters are still unavailable, while in other cases reported data show significant variability and warrant critical re-evaluation.
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