US20250312495
2025-10-09
Human necessities
A61K51/0478
The patent application describes a novel method for radiolabeling biomolecules, such as peptides and sugars, using an organometallic gold(III) complex. This process involves the 18F-labeling of unprotected peptides and sugars through thioarylation with a Au(III)-[18F]fluoroaryl complex. The method is notable for its rapidity, achieving high radiochemical yields within 15 minutes in an aqueous environment, while also demonstrating excellent tolerance to various functional groups. The stability and robustness of the gold(III) complex make it a versatile agent for efficient radiolabeling.
The invention was developed with government support under a grant from the National Institutes of Health, which retains certain rights to the invention. It is intended for use in imaging applications such as positron emission tomography (PET), providing a new approach to the 18F-labeling of biomolecules that overcomes limitations associated with existing methods like 18F-SFB. The traditional 18F-SFB method suffers from unselective conjugation and low radiochemical yields, highlighting the need for more effective materials and methods that this invention aims to fulfill.
Key components of the invention include compositions containing an oxidative addition reagent with gold(III), a ligand bound to gold(III), and an aryl or heterocycle ring linked to an 18F or 11C moiety. These reagents can react with biomolecules containing sulfur or selenium atoms, resulting in covalent linkage of the radiolabel. The invention also encompasses methods for creating these compositions and performing oxidative addition reactions that couple 18F or 11C to biomolecules, enhancing their utility in PET imaging.
The methods described are efficient, typically occurring at temperatures below 45°C and completing within a short timeframe, often less than 15 minutes. The reactions achieve high radiochemical yields, often exceeding 80% or 90%. This efficiency makes the process suitable for generating radiolabeled polypeptides or polysaccharides used in PET imaging, providing a significant advancement in the field by enabling rapid and selective labeling.
Overall, this invention represents a significant step forward in the field of molecular imaging. It leverages the unique properties of organometallic complexes to provide a more effective means of producing radiolabeled compounds for PET scans. This advancement not only addresses current limitations but also opens new possibilities for research and diagnostic applications in medical imaging.