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Synthesis and Evaluation of [64Cu]PSMA-617 Targeted for Prostate-Specific Membrane Antigen in Prostate Cancer
https://repo.qst.go.jp/records/47946
https://repo.qst.go.jp/records/479464cc39ef0-d54f-4ff1-87be-c94c28f9f382
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2017-05-17 | |||||
タイトル | ||||||
タイトル | Synthesis and Evaluation of [64Cu]PSMA-617 Targeted for Prostate-Specific Membrane Antigen in Prostate Cancer | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Cui, Can
× Cui, Can× Hanyu, Masayuki× Hatori, Akiko× Zhang, Yiding× Xie, Lin× Ohya, Tomoyuki× Fukada, Masami× Suzuki, Hisashi× Nagatsu, Kotaro× Jiang, Cuiping× Luo, Rui× Shao, Guoqiang× Zhang, Ming-Rong× Wang, Feng× 破入 正行× 羽鳥 晶子× 張 一鼎× 謝 琳× 大矢 智幸× 深田 正美× 鈴木 寿× 永津 弘太郎× 張 明栄 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | 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. \n |
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書誌情報 |
American Journal of Nuclear Medicine and Molecular Imaging 巻 7, 号 2, p. 40-52, 発行日 2017-04 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | ISSN:2160-8407 |