Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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64Cu-labelled Lipophilic Porphyrin Derivatives for PET Imaging of Brain Tumor

  • Changkeun Im (Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS)) ;
  • Ji-Ae Park (Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS)) ;
  • Choong Mo Kang (Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS))
  • Received : 2023.11.11
  • Accepted : 2023.11.20
  • Published : 2023.12.30
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Abstract

Generally, short half-life radioisotopes, such as 11C and 18F are used in the development of radiopharmaceuticals for the diagnosis of brain disease. Several FDA-approved 11C or 18F-labeled radiopharmaceuticals are applied clinically. However, radiometal-labeled radiopharmaceuticals have not received FDA approval with leaving a gap in the available options for healthcare professionals and patients. Radiometals are attractive radioisotopes, which can be synthesized in a simpler method than halides or carbon and have allowed the advances in both diagnosis and therapy. These advantages prompted the development of a new approach utilizing a hydrophobic porphyrin derivative that incorporated N,N-dimentyl-4-p-phyenylenediamine (DMPD) which has high affinity to tumor and redox active. In this study, we radiolabeled and evaluated porphyrin and 5,10,15,20-(tetra-N,N-diemethyl-4-aminophenyl)porphyrin (TDAP) which was composed of four DMPD conjugated to the porphyrin radiolabeled with radiometal, 64Cu, to confirm their potential as brain tumor diagnostic agents. The radiochemical yield of [64Cu]Cu-porphyrin was 57.2 ± 5.6% and that of [64Cu]Cu-TDAP was 18.7 ± 2.0% and the radiochemical purity was over 95%. The stability of [64Cu]Cu-porphyrin and [64Cu]Cu-TDAP were confirmed over 95% for 24 hours in human and mouse serum. This protocol proposed the method of 64Cu-labeling to hydrophobic porphyrin compounds.

Keywords

Acknowledgement

This research was supported by the National Research Foundation of Korea (NRF) grants funded by the Korean government (MSIT) (No. 50461-2023 and 2021R1F1A1047996). No potential conflicts of interest were disclosed by authors.

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