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Development of a (177)Lu-Labeled RGD Derivative for Targeting Angiogenesis

Cited 11 time in Web of Science Cited 11 time in Scopus
Authors
Ju, Chang Hwan; Jeong, Jae Min; Lee, Yun-Sang; Kim, Young Joo; Lee, Dong Soo; Lee, Myung Chul; Jeong, Seo Young; Chung, June-Key; Lee, Byung Chul
Issue Date
2010-12
Publisher
MARY ANN LIEBERT INC
Citation
CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS; Vol.25 6; 687-691
Keywords
angiogenesisLu-177RGDradionuclide therapyNOTAlutetium
Abstract
Various Arg-Gly-Asp (RGD) derivatives have been labeled with various radioisotopes for targeting alpha(v)beta(3) integrin, which is expressed during angiogenesis in tumor. In this study, 2-(4`-isothiocyanatobenzyl)-1,4,7-triazacyclononane- 1,4,7-triacetic acid (NOTA-SCN) and its c(RGDyK) conjugate (NOTA-SCN-c(RGDyK)) were labeled with (177)Lu, which is a near ideal radionuclide for treating tumors because it emits therapeutic beta particles and gamma rays for monitoring. (177)Lu (250 MBq) was labeled with 50 mu g NOTA-SCN-c(RGDyK) quantitatively. The specific activity of (177)Lu-NOTA-SCN-c(RGDyK) was 1.44 X 10(5) Ci/mol. Biodistribution study was performed in Balb/c mice xenografted with CT-26 (mouse colon cancer) cells. The highest uptake was found in kidneys (7.56% +/- 0.71% ID/g at 1 hour), and tumor uptake was 1.70% +/- 0.33% ID/g at 1 hour postinjection. Moderate tumor-to-blood (2.36 +/- 0.29) and tumor-to-muscle (2.06 +/- 0.40) ratios were observed. This study shows that (177)Lu-NOTA-SCN-c(RGDyK) is a potential therapeutic agent for angiogenic tumors, but special care is required to prevent kidney toxicity.
ISSN
1084-9785
Language
English
URI
http://hdl.handle.net/10371/78266
DOI
https://doi.org/10.1089/cbr.2010.0825
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College of Medicine/School of Medicine (의과대학/대학원)Nuclear Medicine (핵의학전공)Journal Papers (저널논문_핵의학전공)
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