量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum and Radiological Science and Technology.
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PET imaging and quantification of the effects of succinylated gelatin and/or L-lysine on renal uptake and retention of the novel radiopharmaceutical 64Cu-cyclam-RAFT-c(-RGDfK-)4
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Objective: 64Cu-cyclam-RAFT-c(-RGDfK-)4 (64Cu-RAFTRGD) is a novel tetrameric cyclic RGD peptide probe for PET imaging of tumor angiogenesis via targeting the V3 integrin. Because 64Cu also emits -, it can be used for internal radiotherapy. We studied the effects of a succinylated gelatin-containing plasma expander Gelofusine and L-lysine on the renal uptake and retention of 64Cu-RAFTRGD in tumor-bearing mice, aiming to find measures to lower the risk of nephrotoxicity in internal radiotherapy using 64Cu-RAFTRGD.
Methods: Normal or tumor-bearing mice received injection of 64Cu-RAFTRGD with or without co-injection of Gelofusine, L-lysine, or the both. Biodistribution studies were performed at 3 and 24 h post-injection (p.i.). Dynamic PET scans (5 min/frame) were performed at 0-60 min p.i., followed by static PET scans at 3.5 and 24 h p.i. Radio-TLC was done to analyze the radioactive metabolites in blood, urine, liver, and kidney samples at 1 and 24 h p.i.
Results: Co-injection of Gelofusine significantly reduced the renal uptake and retention of 64Cu-RAFTRGD. Although L-lysine alone had no influence on the renal radioactivity accumulation, it showed the tendency to enhance the inhibitory effect of Gelofusine. The uptake of 64Cu-RAFTRGD in the tumors was not influenced by co-injection of Gelofusine or together with L-lysine. Dynamic PET imaging of mice and metabolic analysis of tissue samples clearly showed that Gelofusine did block the renal reabsorption of 64Cu-RAFTRGD, and did not interfere with the metabolism and excretion pathway of the probe.
Conclusion: Administration of Gelofusine or together with L-lysine is a promising measure for kidney protection in internal radiotherapy using 64Cu-RAFTRGD.
PET imaging and quantification of the effects of succinylated gelatin and/or L-lysine on renal uptake and retention of the novel radiopharmaceutical 64Cu-cyclam-RAFT-c(-RGDfK-)4
