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Choi, S.J.; Lee, S.Y.; Park, P.H.; Choi, K.H.; Hong, Y.D., E-mail: Choisj@kaeri.re.kr
Report on the Technical Meeting on Therapeutic Radiopharmaceuticals2009
Report on the Technical Meeting on Therapeutic Radiopharmaceuticals2009
AbstractAbstract
[en] The main goal of this study was to optimize the radioimmunoconjugation of monoclonal antivascular endothelial growth factor receptor 1(VEGFR 1) anti-CD105(Endoglin) monoclonal antibody for an angiogenesis targeting and with 177Lu as a potential angiogenic molecular tracer for radioimmunotherapy (RIT). We carried out a radioimmunoconjugation using 177Lu with anti-CD105 (Endoglin) and anti-VEGFR1 for developing a more useful marker to identify proliferating endothelium involved in tumor angiogenesis than panendothelial markers. We optimized the labeling of monoclonal antibody with 177Lu by using cysteine derivative isothiocyanatobenzyl-DTPA(DTPA-NCS) as BFCA. Under the optimal conditions with a slight modifications on the factors such as the reaction time and molar ratio which are known to be very critical in radiolabeling. The labeling yield was greater than 99% each respectively. Immunoactivity of the radioimmunoconjugate was investigated using combinations of radioanalytical and bioanalytical techniques (ITLC- SG,Cyclone phosphorimager, SDS-PAGE and ELISA). For the biological evaluations we carried out a cell binding assay and a biodistribution study using mice bearing Calu 6 lung cancer cell xenografts. The tumor-to-blood ratio was 11.16:1 24h post-injection. For anti- VEGFR1 monoclonal antibody, the biodistribution study showed high specificity in accumulating in tumour tissues where the tumor-to-blood ratio was 3.25:1 24h post-injection. In conclusion, the anti-CD105 monoclonal antibody for an angiogenesis targeting was effectively radioconjugated with 177Lu. And the biodistribution study showed a high specificity for accumulating in tumour tissues. This radioimmunoconjugate is applicable to detect angiogenesis sites in various diseases and to treat tumors. the anti-VEGFR1 monoclonal antibody for angiogenesis targeting was effectively radioconjugated with 177Lu. This radioimmunoconjugate is applicable to detect of angiogenesis sites in various diseases and treat tumour over expressed VEGFR 1. (author)
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International Atomic Energy Agency, Industrial Applications and Chemistry Section, Vienna (Austria); 113 p; 2009; p. 86; Technical Meeting on Therapeutic Radiopharmaceuticals; Vienna (Austria); 16-20 Nov 2009; Abstract only
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Report
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Conference
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ANIMAL TISSUES, ANTIBODIES, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, BODY, DAYS LIVING RADIOISOTOPES, IMMUNOTHERAPY, INTERMEDIATE MASS NUCLEI, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LUTETIUM ISOTOPES, MEDICINE, MEMBRANE PROTEINS, MITOGENS, NUCLEAR MEDICINE, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, PROTEINS, RADIOISOTOPES, RADIOLOGY, RADIOTHERAPY, RARE EARTH NUCLEI, THERAPY
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