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Radiolabeling and biodistribution of monoclonal antibody (MAb) anti-CD20 with iodine-131

机译:碘131对单克隆抗体(CD20)的放射标记和生物分布

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Radioactive isotopes of iodine, mainly iodine-131 have been broadly used in many monoclonal antibody radioiodination settings, employing different methods. In this study, using a Chloramine-T procedure, the influence of incubation time, CT mass, and Ab/activity ratio on the radiochemical yield of the anti-CD20 antibody labeled with iodine-131 was observed. Radiochemical yield was > 97 %, employing different Chloramine-T masses, independently of incubation time. Radiochemical purity was above 99 % after purification of the labeled compound. The relationship between Ab mass and radioactivity was tested and no difference was observed when 90.6 MBq (2.45mCi) of activity was incorporated in the Ab-mass range studied. Biodistribution study in normal Swiss mice showed higher uptake by the liver and intestines. Low thyroid uptake indicated a suitable in vivo stability. Slight blood uptake was considered a result of circulating radioactivity in normal organs and tissues. A favorable biological distribution of 131I-anti-CD20 suggests this radiopharmaceutical may be effectively used in the therapy of Non Hodgkin Lymphoma.
机译:碘的放射性同位素,主要是碘131,已通过多种方法广泛用于许多单克隆抗体放射性碘化环境中。在这项研究中,使用氯胺T程序观察了孵育时间,CT质量和Ab /活性比对用碘131标记的抗CD20抗体的放射化学产率的影响。放射化学产率> 97%,采用不同的氯胺-T质量,与孵育时间无关。纯化标记化合物后,放射化学纯度高于99%。测试了Ab质量与放射性之间的关系,当在研究的Ab质量范围内掺入90.6 MBq(2.45mCi)的放射性时,没有观察到差异。在正常的瑞士小鼠中进行的生物分布研究表明,肝脏和肠道对它们的摄取更高。甲状腺摄取低表明体内合适。少量血液被认为是正常器官和组织中循环放射性的结果。 131I-抗CD20的良好生物学分布表明,该放射性药物可有效用于非霍奇金淋巴瘤的治疗。

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