Background

Use of radiometals in nuclear oncology is a rapidly growing field that uses the properties of radioactive atoms to create radiopharmaceuticals that treat and diagnose cancer. These radiopharmaceuticals can be broken down into four components containing a radiometal, chelator, linker and bioconjugate/targeting vector. Each component has a specific function, where the radiometal provides the diagnosis/treatment, the bioconjugate/targeting vector ensures accumulation of the drug at the point of infection, while the chelator and linker (defined as bifunctional chelator (BFC)) integrate these two components together. The present invention proposes bifunctional [2.2.2]Cryptand chelators could potentially lead to new ligands that bind radiometals under radiopharmaceutical conditions (vide supra) to form exceptionally thermodynamically stable and kinetically inert complexes in vivo. One challenge would be