Audicio Paola F, Castellano Gustavo, Tassano Marcos R, Rezzano Maria E, Fernandez Marcelo, Riva Eloisa, Robles Ana, Cabral Pablo, Balter Henia, Oliver Patricia
Departamento de Radiofarmacia, Centro de Investigaciones Nucleares, Facultad de Ciencias, Universidad de la República, Mataojo 2055, Montevideo, Uruguay.
Appl Radiat Isot. 2011 Jul;69(7):924-8. doi: 10.1016/j.apradiso.2011.01.026. Epub 2011 Jan 26.
Anti-CD20 (Rituximab®), a specific chimeric monoclonal antibody used in CD20-positive Non-Hodgkin's Lymphoma, was conjugated to a bifunctional quelate (DOTA) and radiolabeled with (177)Lu through a simple method. [(177)Lu]-DOTA-anti-CD20 was obtained with a radiochemical purity higher than 97%, and showed good chemical and biological stability, maintaining its biospecificity to CD20 antigens. Monte Carlo simulation showed high doses deposited on a spheroid tumor mass model. This method seems to be an appropriate alternative for the production of [(177)Lu]-DOTA-anti-CD20 as therapeutic radiopharmaceutical.
抗CD20（利妥昔单抗®）是一种用于CD20阳性非霍奇金淋巴瘤的特异性嵌合单克隆抗体，通过一种简单方法与双功能螯合剂（DOTA）偶联，并使用（177）镥进行放射性标记。获得的[（177）镥]-DOTA-抗CD20放射性化学纯度高于97%，并表现出良好的化学和生物学稳定性，保持其对CD20抗原的生物特异性。蒙特卡罗模拟显示在球形肿瘤块模型上沉积了高剂量。该方法似乎是生产[（177）镥]-DOTA-抗CD20作为治疗性放射性药物的合适替代方法。
