1. Toward Personalized Medicine: One Chelator for Imaging and Therapy with Lutetium-177 and Actinium-225
- Author
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Patrick Cieslik, Manja Kubeil, Kristof Zarschler, Martin Ullrich, Florian Brandt, Karl Anger, Hubert Wadepohl, Klaus Kopka, Michael Bachmann, Jens Pietzsch, Holger Stephan, and Peter Comba
- Subjects
Radioisotopes ,somatostatin analogue ,General Chemistry ,actinium ,Lutetium ,trivalent metal ions ,Biochemistry ,Catalysis ,lutetium ,radionuclide theranostics ,Mice ,Colloid and Surface Chemistry ,Animals ,Humans ,Tissue Distribution ,bispidine ,Precision Medicine ,Radiopharmaceuticals ,Chelating Agents - Abstract
We report a nonadentate bispidine (3,7-diazabicyclo[3.3.1]nonane) that unveils the potential to bind theranostically relevant radionuclides, including indium-111, lutetium-177 and actinium-225 at mild labeling conditions. This radiopharmaceutical candidate allows the simultaneous application of imaging and treatment (radionuclide theranostics) without changing the type of bioconjugate, i.e. it allows the strong binding to an imaging and a therapeutic radionuclide by the same chelator. Since sophisticated coordination chemistry is required to achieve high thermodynamic and kinetic stability, it is not surprising that only a few chelators have been reported that are able to strongly bind several radionuclides to a satisfactory extent. Bispidine-derived ligands have proven to be ideal for di- and trivalent metal ions with generally fast complexation kinetics and high in vitro and in vivo stabilities. The presented (radio)complexes are formed under mild conditions (pH 6
- Published
- 2022