Synthesis and biological evaluation of diagnostic reagent for prostate cancer using copper-64 radioisotope
안희수, 김미현, 한상진, 우상근, 김정영, 이규철, 임일한, 이용진,
소속 상세정보
안희수 ( Ahn Hee-Su )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
김미현 ( Kim Mi-Hyun )
FutureChem Healthcare Co., Ltd.
한상진 ( Han Sang-Jin )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
우상근 ( Woo Sang-Keun )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
김정영 ( Kim Jung-Young )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
이규철 ( Lee Kyu-Chul )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
임일한 ( Lim Il-Han )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
이용진 ( Lee Yong-Jin )
Korea Institute of Radiological and Medical Sciences Division of Applied RI
Abstract
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.
키워드
Prostate cancer; Prostate specific membrane antigen(PSMA); PSMA-617; Cu-64
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