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KMID : 1145520170030020059
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Journal of Radiopharmaceuticals and Molecular Probes
2017 Volume.3 No. 2 p.59 ~ p.64
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Development of bombesin peptide kit for prostate cancer diagnosis and treatment using 64Cu/177Lu.
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Kim Mi-Hyun
Kim Min-Hwan
Kim Kwang-Il
Kim Jung-Young
Lee Tae-Sup
Kang Joo-Hyun
Lee Kyo-Chul
Lee Yong-Jin
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Abstract
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It has been reported that 64Cu was radiolabeled with bombesin (BBN) peptide binding to the gastrin releasing peptide receptor expressed in human prostate cancer cells (PC3), confirming tumor target efficacy in mouse model. In this study, we developed the kit for the diagnosis and treatment of prostate cancer that can be used clinically using bombesin peptide available of 64Cu and 177Lu radioisotope labeling. The NODAGA-galactoBBN peptide containing the NODAGA chelator and galactose was dispensed into a sterilized glass vial and lyophilized to prepare a kit. The stability of the kit after long-term storage in the 4˚C cold chamber and the radiolabeling efficiency after 64Cu or 177Lu labeling were confirmed by thin layer chromatography. When labeling with 64Cu at the initial stage of storage, labeling efficiency of NODAGA-galacto-BBN peptide kit was over 96%, labeling efficiency was over 90% when 177Lu was labeled. At 11 months after storage, the radiolabeling efficiency of kit against 64Cu and 177Lu was each over 95% and 90%. The cell viability was significantly reduced in the 177Lu-NODAGA-galacto-BBN treated group compared with the control and 177Lu alone treated group in clonogenic assay. In conclusion, the NODAGA-galacto-BBN kit prepared by the lyophilization showed high stability over time and high yield of radioisotope labeling. Also 177Lu-NODAGA-galacto-BBN confirmed high cytotoxicity to prostate cancer cells. Therefore, the NODAGA-galacto-bombesin kit is expected to be useful for the diagnosis and treatment of prostate cancer patients.
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KEYWORD
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64Cu, 177Lu, bombesin, NODAGA, PC3, prostate cancer
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