Sc-HOPO: A Potential Construct for Use in Radioscandium-Based Radiopharmaceuticals

Inorg Chem. 2023 Dec 18;62(50):20567-20581. doi: 10.1021/acs.inorgchem.2c03931. Epub 2023 Feb 1.

Abstract

Three isotopes of scandium─43Sc, 44Sc, and 47Sc─have attracted increasing attention as potential candidates for use in imaging and therapy, respectively, as well as for possible theranostic use as an elementally matched pair. Here, we present the octadentate chelator 3,4,3-(LI-1,2-HOPO) (or HOPO), an effective chelator for hard cations, as a potential ligand for use in radioscandium constructs with simple radiolabeling under mild conditions. HOPO forms a 1:1 Sc-HOPO complex that was fully characterized, both experimentally and theoretically. [47Sc]Sc-HOPO exhibited good stability in chemical and biological challenges over 7 days. In healthy mice, [43,47Sc]Sc-HOPO cleared the body rapidly with no signs of demetalation. HOPO is a strong candidate for use in radioscandium-based radiopharmaceuticals.

MeSH terms

  • Animals
  • Chelating Agents / chemistry
  • Ligands
  • Mice
  • Positron-Emission Tomography / methods
  • Pyridones* / chemistry
  • Radiopharmaceuticals* / chemistry

Substances

  • Radiopharmaceuticals
  • Pyridones
  • Chelating Agents
  • Ligands