Backbone-Substituted Bifunctional DOTA Ligands, Complexes and Compositions Thereof, and Methods of Using the Same
Description of Invention:
The subject technology is directed to three backbone-substituted 1,4,7,10-tetraazacyclododecane (DOTA) compounds. These compounds can be chelated with radionuclides and used as imaging or therapeutic agents. In particular, the compounds can be complexed with a paramagnetic element (e.g. Gd (III)) and used as contrast agents in magnetic resonance imaging (MRI) applications.
The DOTA derivatives of the invention are such that the macrocyclic backbone was pre-arranged or pre-organized in order to lower the energy barrier to complex formation, thereby potentially increasing the rate of complex formation. The pre-organization and macrocyclic effect of the DOTA sub-structure accelerates complexation with metal ions and isotopes (e.g. Y (III), Gd (III); etc.), while maintaining a high level of stability of the complexes.
Inventors:
Martin Brechbiel (NCI) Hyun-Soon Chong (NCI)
