169237-39-2Relevant articles and documents
RADIO-PHARMACEUTICAL COMPLEXES
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Page/Page column 32; 43; 44, (2017/10/18)
The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a
Alpha-emitting complexes
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Page/Page column 37, (2017/10/18)
The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.
An efficient chelator for complexation of thorium-227
Ramdahl, Thomas,Bonge-Hansen, Hanne T.,Ryan, Olav B.,Larsen, ?smund,Herstad, Gunnar,Sandberg, Marcel,Bjerke, Roger M.,Grant, Derek,Brevik, Ellen M.,Cuthbertson, Alan S.
supporting information, p. 4318 - 4321 (2016/08/18)
We present the synthesis and characterization of a highly efficient thorium chelator, derived from the octadentate hydroxypyridinone class of compounds. The chelator forms extremely stable complexes with fast formation rates in the presence of Th-227 (ambient temperature, 20?min). In addition, mouse biodistribution data are provided which indicate rapid hepatobiliary excretion route of the chelator which, together with low bone uptake, supports the stability of the complex in vivo. The carboxylic acid group may be readily activated for conjugation through the ?-amino groups of lysine residues in biomolecules such as antibodies. This chelator is a critical component of a new class of Targeted Thorium Conjugates (TTCs) currently under development in the field of oncology.