Prostate cancer (PCa) is the second most common type of cancer diagnosed in men worldwide. Prostate specific membrane antigen (PSMA) is a transmembrane protein that is highly expressed in PCa tumors and provides a reliable target for PCa imaging. Positron emission tomography (PET) with tracers targeting PSMA has proven to be a promising avenue for non-invasive and reliable imaging of disease. Effective small molecule PSMA targeting ligands have been previously developed but exhibit non-ideal characteristics for theranostic applications. The availability of scandium and copper imaging and therapy isotopes (44/47Sc, 64/67Cu) enables an “apples-to-apples” comparison of imaging and therapy modality. This renders copper and scandium an attractive avenue for theranostic approaches to prostate cancer imaging. We have developed, synthesized, and characterized radiometal chelators for scandium, copper, and lutetium and appended for PSMA targeting for the imaging and treatment of prostate cancer. Based on a picolinate-functionalized triazamacrocycle, these chelators demonstrate rapid complexation with radiometals of interest and have been characterized by spectroscopic and radiochemical experiments as kinetically inert and suitable for in vivo application. PET-imaging and biodistribution studies have established picaga-DUPA as an ideal choice for using the 44Sc PET nuclide. In pilot studies, mice with PSMA-expressing xenografts exhibited significantly diminished tumor growth upon a single treatment with 47Sc-(picaga)-DUPA or 177Lu-(picaga)-DUPA compared to vehicle only.

Radiometal-based small molecule tracers for prostate cancer

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.