The present invention relates to novel compounds as well as to compositions, methods, and kits comprising the compounds for determining an alkyltransferase (ATase), in particular an alkylguanine-DNA alkyl transferase (AGT). In general, the novel compounds provide for determining ATase levels, in particular for in vivo applications including, but not limited to, theranostic applications, in particular to cancer-related applications.
- Durnam NC, US Ganesan VAIDYANATHAN - Chapel Hill NC, US Zhengyuan ZHOU - Durham NC, US
International Classification:
A61K 51/04 A61K 51/10 C07B 59/00 C07D 401/12
Abstract:
The application is drawn to F-radiolabeled residualizing agents and biomolecules and methods for radiolabeling biomolecules with radioactive fluorine atoms. The biomolecules have an affinity for particular types of cells and may specifically bind a certain cell, such as a cancer cell. Relevant biomolecules include antibodies, monoclonal antibodies, antibody fragments, peptides, other proteins, nanoparticles and aptamers. The application further provides compositions including such labeled biomolecules, as well as methods of using the labeled biomolecules and/or compositions in imaging applications.
Radiohalogen Prosthetic Moieties And Radiolabeled Biomolecules
- Durham NC, US Ganesan Vaidyanathan - Chapel Hill NC, US Darryl Lynn McDougald - Durham NC, US
International Classification:
C07B 59/00 C07F 7/22 C07K 16/30 A61K 47/68
Abstract:
The application is drawn to radiohalogen prosthetic moieties and precursors thereof and to radiolabeled biomolecules comprising such radiohalogen prosthetic moieties. The biomolecules have an affinity for particular types of cells and may specifically bind a certain cell, such as a cancer cell. Relevant biomolecules include antibodies, monoclonal antibodies, antibody fragments, peptides, other proteins, nanoparticles, aptamers, and pharamacological moieties used to target prostate-specific membrane antigen (PSMA).
Psma Targeted Radiohalogenated Urea-Polyaminocarboxylates For Cancer Radiotherapy
- Baltimore MD, US - Durham NC, US Vivek Kumar - Rensselaer NY, US Sangeeta Ray - Ellicott City MD, US Michael Zalutsky - Chapel Hill NC, US Ganesan Vaidyanathan - Chapel Hill NC, US
International Classification:
A61K 51/04 A61P 35/00
Abstract:
Small molecule radiohalogenated PSMA inhibitors and metal complexes thereof and their use in radioimaging and radiotherapy for treating PSMA-related diseases, including prostate cancer, are disclosed. The combination of small molecule radiohalogenated PSMA inhibitors with a competitive PSMA ligand for reducing off target accumulation of the radiohalogenated PSMA inhibitor also is disclosed.
Psma Targeted Radiohalogenated Ureas For Cancer Radiotherapy
- BALTIMORE MD, US - DURHAM NC, US YING CHEN - LUTHERVILLE-TIMONIUM MD, US SANGEETA RAY - ELLICOTT CITY MD, US MICHAEL ZALUTSKY - CHAPEL HILL NC, US GANESAN VAIDYANATHAN - CHAPEL HILL NC, US
International Classification:
C07F 13/00 A61P 35/00
Abstract:
PPSMA binding scaffolds with radioiodinated, radiobrominated and radioastatinated labeled prosthetic groups are disclosed. Pharmaceutical compositions and methods of treating PSMA expressing cells or tumors also are disclosed.
- Durham NC, US Ganesan Vaidyanathan - Chapel Hill NC, US
International Classification:
A61K 51/10 A61K 51/04 A61P 35/00
Abstract:
The application is drawn to radiolabeled biomolecules and methods for radiolabeling biomolecules with radioactive halogen atoms that minimizes loss of the radioactive halogen due to dehalogenation in vivo, preserves the biological activity of the biomolecule, maximizes retention of radioactivity in cancer cells, and minimizes the retention of radioactivity in normal tissues after in vivo administration. Some such radiolabeled biomolecules comprise a radioactive metal atom in place of, or in addition to the radioactive halogen. The biomolecules have an affinity for particular types of cells and may specifically bind a certain cell, such as cancer cells. Relevant biomolecules include antibodies, monoclonal antibodies, antibody fragments, peptides, other proteins, nanoparticles and aptamers.
Prosthetic Compounds For Labeling Internalizing Biomolecules
- Durham NC, US Ganesan Vaidyanathan - Chapel Hill NC, US
International Classification:
A61K 51/10 C07B 59/00 C07D 487/04 C07D 403/12
Abstract:
Prosthetic compounds are disclosed that are effective for radiolabeling biomolecules with 18F. Representative biomolecules include antibodies (e.g., monoclonal antibodies (mAbs) and nanobodies (sdAbs)), antibody fragments, and peptides that may have an affinity for particular types of cells, such as cancer cells. The prosthetic compounds effectively address the art-recognized difficulties associated with the retention of radioactivity within the targeted cells, due to internalization of the biomolecule, followed by proteolytic degradation. Representative prosthetic compounds include (i) a succinimidyloxycarbonyl moiety, (ii) a radioactive moiety bearing 18F, and (iii) a charged moiety, i.e., a moiety that is charged under the physiological conditions of the internal cell environment.