posted on 2023-02-01, 17:37authored byMichael
D. Phipps, Shelbie Cingoranelli, N. V. S. Dinesh
K. Bhupathiraju, Ali Younes, Minhua Cao, Vanessa A. Sanders, Michelle C. Neary, Matthew H. Devany, Cathy S. Cutler, Gustavo E. Lopez, Shefali Saini, Candace C. Parker, Solana R. Fernandez, Jason S. Lewis, Suzanne E. Lapi, Lynn C. Francesconi, Melissa A. Deri
Three isotopes of scandium43Sc, 44Sc, and 47Schave 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.