@article{oai:repo.qst.go.jp:00047247,
 author = {Jin, Zhao-Hui and Furukawa, Takako and Sogawa, Chizuru and Claron, Michael and Aung, Winn and B, Tsuji Atsushi and Wakizaka, Hidekatsu and Zhang, Ming-Rong and Boturyn, Didier and Dumy, Pascal and Fujibayashi, Yasuhisa and Saga, Tsuneo and 金 朝暉 and 古川 高子 and Ｕ Ｗｉｎｎ Ａｕｎｇ and 辻 厚至 and 脇坂 秀克 and 張 明栄 and 藤林 康久 and 佐賀 恒夫},
 issue = {3},
 journal = {European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V},
 month = {Dec},
 note = {(64)Cu-cyclam-RAFT-c(-RGDfK-)4, an αVβ3 integrin-targeting tetrameric cyclic RGD peptide probe, is a potential theranostic compound for positron emission tomography (PET) of tumor angiogenesis and for internal radiotherapy owing to the multiple decay modes of (64)Cu. Since kidneys are dose-limiting organs in internal radiotherapy, we aimed to reduce the renal accumulation of (64)Cu-cyclam-RAFT-c(-RGDfK-)4 by co-injection with Gelofusine (GF), a succinylated gelatin solution, and/or l-lysine (Lys), and to explore, for the first time, the related mechanisms using the noninvasive and quantitative PET imaging technology. Biodistribution assays, dynamic and static PET scans, and metabolism studies with radio-thin-layer chromatography (radio-TLC) were performed in healthy or αVβ3-positive tumor-bearing mice. In the results, co-injection with GF markedly reduced the renal uptake and slightly increased the tumor uptake of (64)Cu-cyclam-RAFT-c(-RGDfK-)4. l-Lysine alone had no effect on the probe biodistribution, but the combined use of Lys and GF tended to enhance the effect of GF. Dynamic PET and metabolite analysis by radio-TLC highly revealed that GF blocks the renal reabsorption of (64)Cu-cyclam-RAFT-c(-RGDfK-)4, but does not interfere with its metabolism and excretion. In conclusion, administration of GF and Lys is a useful strategy for kidney protection in (64)Cu-cyclam-RAFT-c(-RGDfK-)4-based internal radiotherapy.},
 pages = {478--486},
 title = {PET imaging and biodistribution analysis of the effects of succinylated gelatin combined with L-lysine on renal uptake and retention of (64)Cu-cyclam-RAFT-c(-RGDfK-)4 in vivo.},
 volume = {86},
 year = {2013}
}