188Re直接标记单克隆抗体TGLA及其生物学评价

Direct Labeling of Monoclonal Antibody TGLA with 188Re and Biological Evaluation

  • 摘要: 单克隆抗体TGLA是一种特异性靶向CD20的嵌合抗体,能有效杀伤肿瘤细胞和抑制肿瘤细胞增长,已用于B细胞淋巴瘤的临床治疗。本研究采用直接标记法,制备188Re-TGLA,并优化了标记条件。在最佳标记条件下,标记率可达93%,体外放置24 h后,放化纯度≥85%,体外稳定性良好。荷淋巴瘤裸鼠体内分布结果表明,188Re-TGLA在肿瘤的摄取较高,在24 h时为(6.46±2.01)ID%/g,提示188Re-TGLA可以作为一种有效的显像剂,但是为了更好的显像效果,可使用抗体片段进行标记,以缩短抗体的体内半衰期,更好地与188Re匹配。

     

    Abstract: Monoclonal antibody TGLA is a specific targeting CD20 chimeric antibody. It can kill tumor cells and inhibit tumor cells’ growth effectively, which has been applied to clinical therapy of lymphoma cell B. Monoclonal antibody TGLA was labeled with 188Re, directly and got the target compound 188Re-TGLA. Moreover, this work improved the reduction conditions and labeling conditions of 188Re. The labeling yield reached as high as 93% at the optimum conditions. The vitro stability was good with the radiochemical purity of more than 85% after 24 hours in vitro. The biodistribution of the 188Re-TGLA in lymphoma bearing nude mice showed high uptake in tumor ((6.46±2.01)ID%/g, 24 h), implied that 188Re-TGLA can be used for imaging effectively. However,in order to get better imaging, antibody fragment with short half life in vivo should be used for labeling of 188Re.

     

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