Chelator Design and Radiolabeling Chemistry of Radiometals

The design and synthesis of radiopharmaceuticals is a prime example of interdisciplinary research. Radiometal-based pharmaceuticals have become the subject of significant interest due to the wide variety of available radionuclides with suitable decay characteristics for theragnostic applications. However, the synthesis of these precision radiopharmaceuticals is not without challenges. This chapter provides a whistlestop tour of essential principles in metal–ligand co-ordination chemistry with the aim of outlining the characteristic traits of metal ions, chelators and targeting vectors, as well as their intricate combinations as theragnostic agents to diagnose and treat a widening array of disease pathologies. We also briefly discuss the experimental parameters and determinants of good radiolabeling protocol. Lastly, we contextualize these concepts with a spotlight selection of promising metal-based radiopharmaceuticals currently in use and development.