Technology - Triazamacrocycle-derived Chelators for the Coordination of Imaging and Therapy Metal Ions

Triazamacrocycle-derived Chelators for the Coordination of Imaging and Therapy Metal Ions

Rapid and inert radiolabeling with an array of radioactive isotopes suitable for medical imaging and therapy approaches.

Background:

Personalized medicine, or individually tailored patient treatment, is an emerging clinical management paradigm. In nuclear medicine, this entails exploiting diagnostic techniques, such as non-invasive imaging by means of Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT), to modify radiotherapeutic treatment regimes. If the same drug is labeled with a diagnostic and a therapeutic radionuclide for sequential imaging and treatment, the approach is considered “theranostic.” Theranostic isotope pairs enable diagnostic imaging that is directly, accurately and reliably predictive of therapy and imaging can be carried out for prolonged periods of time. However, in order to utilize metallic theranostic isotope pairs, customized chelation approaches are required that enable targeted delivery of isotope payload to the site of interest.

Technology Overview:

⁴⁴Scandium and ⁶⁴copper have recently emerged as an attractive, short-lived, PET isotopes with a matched radiotherapeutic isotope for radio therapy (⁴⁷Sc, ⁶⁷Cu, ¹⁷⁷Lu). In this invention, novel, modular chemical entities with high affinity to copper, scandium and lutetium radioisotopes and a freely functionalizable moiety have been synthesized. These constructs are suitable to kit-type formulations for single-step radiochemical synthesis of diagnostic and therapeutic entities radiolabeled with scandium, copper and lutetium isotopes, and are readily suitable for applications using other any desirable targeting vectors of peptidic/small molecule, protein or antibody nature.

Advantages:

This technology allows for rapid and inert radiolabeling with an array of radioactive isotopes suitable for imaging and therapy approaches. This renders the technology superior to currently commercially available ¹⁸F-, ⁶⁸G-, and ¹⁷⁷Lu-based tracers.