Recent Advances in Zirconium-89 Chelator Development

The interest in zirconium-89 ((89)Zr) as a positron-emitting radionuclide has grown considerably over the last decade due to its standardized production, long half-life of 78.2 h, favorable decay characteristics for positron emission tomography (PET) imaging and its successful use in a variety of clinical and preclinical applications. However, to be utilized effectively in PET applications it must be stably bound to a targeting ligand, and the most successfully used (89)Zr chelator is desferrioxamine B (DFO), which is commercially available as the iron chelator Desferal(®). Despite the prevalence of DFO in (89)Zr-immuno-PET applications, the development of new ligands for this radiometal is an active area of research. This review focuses on recent advances in zirconium-89 chelation chemistry and will highlight the rapidly expanding ligand classes that are under investigation as DFO alternatives.