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KMID : 1145520180040020065
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Journal of Radiopharmaceuticals and Molecular Probes
2018 Volume.4 No. 2 p.65 ~ p.72
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Synthesis and biological evaluation of diagnostic reagent for prostate cancer using copper-64 radioisotope
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Ahn Hee-Su
Kim Mi-Hyun
Han Sang-Jin
Woo Sang-Keun
Kim Jung-Young
Lee Kyu-Chul
Lim Il-Han
Lee Yong-Jin
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Abstract
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Prostate specific membrane antigen (PSMA) is a cell surface membrane protein, which is overexpressed in most prostate cancer. Recently, PET imaging with [68Ga]PSMA-HBED-CC has been widely used for the diagnosis of recurrent prostate cancer and the studies on the diagnostic potential of 64Cu-labeled PSMA ligands reported actively. In this study, we monitored with biological evaluation in vivo and PET imaging of 64Cu-labeled PSMA ligand ([64Cu]PSMA-617). The radiolabelling efficiency and stability of [64Cu]PSMA-617 were confirmed by radio-thin layer chromatography. The radiolabeling efficiency of [64Cu]PSMA-617 showed over 95%, and stabilities of intact remained over 98% in both human and mouse serum for 48 h. In normal male mice, in vivo uptake of [64Cu]PSMA-617 in several organs was measured at 2, 4, 6, 24, 48 h after injection. Rapid blood clearance was observed for [64Cu]PSMA-617. The high uptake was observed in the lung, liver, intestines and kidneys at 2 h postinjection, but was low in the other organs (1-2 %ID/g) at 4 h. The dynamic PET/CT images of 22RV1 tumor-bearing nude mice were acquired during 60 min and additionally acquired 24 h and 48 h after injection. In dynamic PET images, [64Cu]PSMA-617 uptake ratio in tumors versus muscle was increased as time elaplsed until 60 minutes and remained in tumors at 48 h. In these results, the PET/CT imaging using [64Cu]PSMA-617 in prostate cancer is expected to be useful for the diagnosis and treatment of prostate cancer patients.
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KEYWORD
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Prostate cancer, Prostate specific membrane antigen(PSMA), PSMA-617, Cu-64
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