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A new bifunctional chelator for copper radiopharmaceuticals : a cage amine ligand with a carboxylate functional group for conjugation to peptides

This paper describes the first bifunctional sarcophagine ligand conjugated to a peptide for PET diagnostic imaging using the isotope, copper-64. Biological conjugates of this ligand can be rapidly labelled with copper-64 at low conjugate concentrations in quantitative yield and high purity under ambient conditions, and the resulting PET tracer has excellent stability in vivo. Combined, these properties result in (i) simplified radiopharmaceutical synthetic procedures and (ii) high PET image quality. This research resulted in intellectual property that is currently under license, and the bifunctional sarcophagine ligand is now commercially available from Clarity Pharmaceuticals Ltd.