Theranostic radiometals such as mercury-197m/g (197m/gHg, t1/2 = 23.8 h/64.1 h) continue to attract interest as the incorporation of these radionuclides in radiopharmaceuticals have profound potential to both image (diagnostic SPECT imaging via gamma-ray decay emissions) and treat diseases such as cancer (therapeutic radiation via Auger electrons) simultaneously, using the same drug construct. The literature surrounding 197m/gHg radiopharmaceuticals is limited. Particularly, the underdevelopment of selective and stable bifunctional chelators (BFCs) for 197m/gHg prevents its use in clinical radiopharmaceuticals. In this study, BFCs that efficiently coordinate to 197m/gHg for incorporation into radiopharmaceuticals are identified by screening commercially available and novel sulfur-rich BFCs. This work includes novel ligand design and synthesis, followed by complex characterization and the determination of the radiochemical conversion for these ligands with 197m/gHg.

Development and exploration of bifunctional chelating ligands for mercury-197m/g

ACS Spring Meeting 2021

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