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Preliminary Preparation of 177Lu-Labeled Rituximab |
MA Xiu-feng1, ZHANG Jun-li3, Li Hong-yu2,3, GAO Shuai3, DU Jin2,4 |
1. Beijing Radiation Safety Technology Center, Beijing 100089 China; 2. Department of Isotopes, China Institute of Atomic Energy; 3. HTA CO., Ltd. ; 4. China Isotope & Radiation Corporation |
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Abstract Objective For confirming the optimal labeling condition, Rituximab was conjugated to two bifunctional chelating agents (p-SCN-Bz-DOTA and p-SCN-Bz-DTPA), and the conjugates were radiolabeled with 177Lu.Methods Rituximab was conjugated to the chelating agents, then the conjugates were radiolabeled with 177Lu. The amount of antibody, nuclide and buffer were fixed, this work emphasized the investigation of PH, reaction time, temperature and the amount of chelating agents.Results conjugates were obtained with labeling yield between 3% to 99.9% at different labelling conditions, the preliminary work demonstrated that the optimum labeling conditions were the reaction molar ratio of monoclonal antibody and chelating agent was 1:100, pH=6.0~7.0, reacting at 40℃ for 30 min.Conclusion Conjugates were obtained with labeling yield and radiochemical purity higher than 99% at optimum labelling conditions, it could be suitable for clinical research.
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Received: 13 January 2016
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