1. Sc-HOPO: A Potential Construct for Use in Radioscandium-Based Radiopharmaceuticals.
- Author
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Phipps MD, Cingoranelli S, Bhupathiraju NVSDK, Younes A, Cao M, Sanders VA, Neary MC, Devany MH, Cutler CS, Lopez GE, Saini S, Parker CC, Fernandez SR, Lewis JS, Lapi SE, Francesconi LC, and Deri MA
- Subjects
- Animals, Mice, Chelating Agents chemistry, Positron-Emission Tomography methods, Ligands, Radiopharmaceuticals chemistry, Pyridones chemistry
- Abstract
Three isotopes of scandium─
43 Sc,44 Sc, and47 Sc─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. [47 Sc]Sc-HOPO exhibited good stability in chemical and biological challenges over 7 days. In healthy mice, [43,47 Sc]Sc-HOPO cleared the body rapidly with no signs of demetalation. HOPO is a strong candidate for use in radioscandium-based radiopharmaceuticals.- Published
- 2023
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