Synthesis of Polyamino-Carboxylate Scaffolds for Biological and Biomedical Applications

Noninvasive techniques for disease imaging and targeted therapy allow for personalized treatment regimens. Radiometal-based imaging and therapeutic agents are expanding due to the increasing availability of 64Cu, 89Zr, 55Co, and other isotopes. When coupled to an antibody or other targeting group using an appropriate bifunctional chelator, clinicians can view the localization of the radiopharmaceutical and monitor disease progression using Positron Emission Tomography. Each isotope requires a different chelator to properly bind the radiometal. When translating a compound from the benchtop to the clinic, any change in chelator requires a completely new set of tests to determine safety and efficacy. Here, we developed a panel of chelators capable of binding radiometals used in both imaging and therapeutics. These multi-use chelators pave the way for the application of a single compound for both cancer detection and targeted therapy, thereby speeding clinical development and enhancing patient outcomes.