@article{oai:repo.qst.go.jp:00047946,
 author = {Cui, Can and Hanyu, Masayuki and Hatori, Akiko and Zhang, Yiding and Xie, Lin and Ohya, Tomoyuki and Fukada, Masami and Suzuki, Hisashi and Nagatsu, Kotaro and Jiang, Cuiping and Luo, Rui and Shao, Guoqiang and Zhang, Ming-Rong and Wang, Feng and 破入 正行 and 羽鳥 晶子 and 張 一鼎 and 謝 琳 and 大矢 智幸 and 深田 正美 and 鈴木 寿 and 永津 弘太郎 and 張 明栄},
 issue = {2},
 journal = {American Journal of Nuclear Medicine and Molecular Imaging},
 month = {Apr},
 note = {We radiolabeled a ligand, PSMA-617, of prostate-specific membrane antigen (PSMA) with copper-64 (64Cu), to evaluate the metabolism, biodistribution, and potential of [64Cu]PSMA-617 for PET imaging of prostate cancer. [64Cu]PSMA-617 was synthesized by heating PSMA-617 with [64Cu]CuCl2 in buffer solution at 90 °C for 5 min. In vitro uptake was determined in two cell lines of prostate cancer. In vivo regional distributions were determined in normal and tumor-bearing mice. High radiolabeling efficiency of 64Cu for PSMA-617 yielded [64Cu]PSMA-617 with >99% radiochemical purity. In vitro cellular uptake experiments demonstrated the specificity of [64Cu]PSMA-617 for PSMA-positive LNCaP cells. Biodistribution observations of normal mice revealed high uptake of radioactivity in the kidney and liver. PET with [64Cu]PSMA-617 visualized tumor areas implanted by PSMA-positive LNCaP cells in the mice. Two hours after the injection of [64Cu]PSMA-617 into mice, a radiolabeled metabolite was observed in the blood, liver, urine, and LNCaP tumor tissues. [64Cu]PSMA-617 was easily synthesized, and exhibited a favorable biodistribution in PSMA-positive tumors. Although this radioligand shows slow clearance for kidney and high liver uptake, change of its chelator moiety and easy radiolabeling may enable development of new 64Cu or 67Cu-labeled PSMA ligands for imaging and radiotherapy. 
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 pages = {40--52},
 title = {Synthesis and Evaluation of [64Cu]PSMA-617 Targeted for Prostate-Specific Membrane Antigen in Prostate Cancer},
 volume = {7},
 year = {2017}
}