Garcia Maria Fernanda, Camacho Ximena, Calzada Victoria, Fernandez Marcelo, Porcal Williams, Alonso Omar, Gambini Juan Pablo, Cabral Pablo
Laboratorio de Radiofarmacia, CIN, Montevideo, Uruguay.
Curr Radiopharm. 2012 Jan;5(1):59-64. doi: 10.2174/1874471011205010059.
The Epidermal growth factor receptor (EGFR) family plays an important role in carcinogenesis. CIMAher® (Nimotuzumab), is a humanized monoclonal antibody, which recognizes EGFR with high affinity. The aim of this work was to perform the direct labeling of Nimotuzumab with [99mTc(CO)3(H2O)3]+ as precursor and to evaluate its labeling conditions, in vitro and in vivo stability and biodistrution in normal C57 BL/6J mice. 99mTc(CO3)-Nimotuzumab labeling yields were up to 90%. More than 90% of the complex remained intact after 24 h of incubation with L-Histidine (1/300 molar ratio). Biodistribution studies in normal mice were also performed. Inmunoreactivity was confirmed by cell binding assays with A431cells. These results encourage the evaluation of the potential role of 99mTc(CO)3-Nimotuzumab as a novel tumor-avid radiotracer for targeting in vivo EGFR expression.
表皮生长因子受体（EGFR）家族在肿瘤发生过程中发挥着重要作用。西妥昔单抗（Nimotuzumab）是一种人源化单克隆抗体，它能高亲和力地识别EGFR。本研究的目的是以[99mTc(CO)3(H2O)3]+作为前体对西妥昔单抗进行直接标记，并评估其标记条件、体外和体内稳定性以及在正常C57 BL/6J小鼠体内的生物分布。99mTc(CO3)-西妥昔单抗的标记产率高达90%。与L-组氨酸（摩尔比1/300）孵育24小时后，超过90%的复合物保持完整。还对正常小鼠进行了生物分布研究。通过与A431细胞进行细胞结合试验证实了免疫反应性。这些结果促使人们评估99mTc(CO)3-西妥昔单抗作为一种新型肿瘤亲和放射性示踪剂用于体内靶向EGFR表达的潜在作用。
