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

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

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 as defined by principles of “personalized medicine”; for such utilizations, also the term “theranostics” is used. 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”, or “chelators”) forming a stable complex which is not decomposed in body.


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.


New features:

  • completely new chelator family for copper radioisotopes

  • syntheses of bifunctional chelator with various reactive groups for conjugation reactions

  • synthetic precursor syntheses also patented

  • conjugation reactions were tested

  • radiolabelling with 64-copper is efficient (room temperature, small chelator excess) leading to a high specific activity

  • conjugation reaction conditions tested in water or water-organic solvent mixtures

  • click conjugation reactions tested


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Poslední změna: 21. leden 2018 23:47 
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Univerzita Karlova

Ovocný trh 560/5

Praha 1, 116 36

Česká republika


Identifikátor datové schránky: piyj9b4

IČO: 00216208 

DIČ: CZ00216208


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