AI Article Synopsis
- The development of theranostic agents using alpha emitters addresses a significant clinical need, focusing on combining therapeutic and diagnostic functions in medicine.* -
- A new ligand, macropa-F, was created to effectively bind to alpha therapeutic radiometals, and its properties were tested with lead-203 and bismuth-207 as substitutes for actual alpha-emitting isotopes.* -
- The resulting fluorine-18 and radiometal complexes demonstrated high stability in human serum for several days, showcasing a promising approach for theranostic applications in medicine.*
Article Abstract
The development of theranostic agents for radiopharmaceuticals based on therapeutic alpha emitters marks an important clinical need. We describe a strategy for the development of theranostic agents of this type the functionalization of the ligand with the diagnostic radionuclide fluorine-18. An analogue of macropa, an 18-membered macrocyclic chelator with high affinity for alpha therapeutic radiometals, was synthesized and its complexation properties with metal ions were determined. The new macropa-F ligand was used for quantitative radiometal complexation with lead-203 and bismuth-207, as surrogates for their alpha-emitting radioisotopes. As a diagnostic partner, a radiofluorinated macropa ligand was used for quantitative bismuth(III) and lead(II) complexation. All fluorine-18 and radiometal complexes are highly stable in human serum over several days. This study presents a new proof-of-principle approach for developing theranostic agents based on alpha-emitting radionuclides and fluorine-18.
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Source |
|---|---|
| http://dx.doi.org/10.1039/d4cc04165h | DOI Listing |
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11649299 | PMC |
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