Bifunctional cyclam based ligands for conjugations with targeting vectors and their 64-Cu radiopharmaceuticals for PET imaging

Technology description

The name of the technology: Bifunctional cyclam based ligands for conjugations with targeting vectors and their 64-Cu radiopharmaceuticals for PET imaging
Challenge: Wide range of radioisotopes is used in nuclear medicine for diagnostic and therapeutic applications. In the recent years, a number of metal radioisotopes have been considered as they enable nuclear medicine utilizations exactly according to patient needs. These radioisotopes cannot be applied in a free form as, in such form, they are non-specifically deposited in tissues. Therefore, the metal radioisotopes must be bound by suitable organic compounds (ligands) forming a stable complex.
Description: Copper-64 is emerging PET radioisotope with half-life ~12 h and soft positron emission. Cyclam based ligands (= chelators), as highly selective chelators for copper over metallic impurities (e.g. nickel and zinc), were modified with a highly hydrophilic bis(phosphinate) pendant arm. Bifunctional chelators containing carboxylic, amine, isothiocyanate, azide or cyclooctyne groups were synthesized and conjugated to various substrates and biologically active targeting molecules (oligopeptides, antibodies or their fragments, folic acid, bis-phosphonates etc.). The chelators and their conjugates incorporate 64-Cu very efficiently even at room temperature and with very low chelator excess, producing radiopharmaceuticals with very high specific activities. The 64-Cu-labelled molecules are stable in-vivo with no non-specific deposition of the radiometal and easily excreted from body. The chelators represents a novel and unique family of ligands which has the best labelling efficiency among published copper chelators.
Commercial opportunity: The presented cyclam based ligands combined with copper radioisotopes can be used for visualization of biodistribution of many biologically active compounds using PET imaging. By leveraging this novel theranostic approach, our compounds allow the determination of dose during the diagnostic stage with Copper-64 and delivers the right amount of radiation to the tumor for therapy with Copper-67.
IP protection status: International Patent Application published under PCT
Development status:

Phase 2

Corresponds with TRL 3 and TRL 4

Feasibility study. There is a realistic design of the technology and the initial tests in the laboratory are leading to the specification of the technology requirements and its capabilities.

  • TRL 3 represents a complete idea of a technology with the design of concrete steps, tests and experiments that will need to be carried out to verify that the idea is realistic
  • TRL 4 is a verification of functionality in the laboratory. The result of TRL 4 is the so-called Proof-of-Concept. Technology is therefore designed and tested for its functionality under limited conditions
Partnering strategy: Collaboration licensing
More information: The group is able to prepare the bifunctional chelators up to a gram scale (if required) or to design/synthesize chelators tailored for a particular utilization.
Samples for radiolabelling tests are available on demand (MTA required).
Images: No picture inserted
Keywords: chelators imaging ligands oncology Radiopharmaceuticals
Categories: Pharma Diagnostics
Owner of a technology:
Institution: Charles University
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