Rasaneh Samira, Rajabi Hossein, Babaei Mohammad Hossein, Daha Fariba Johari, Salouti Mojtaba
Department of Medical Physics, Tarbiat Modares University, Tehran, Iran.
Nucl Med Biol. 2009 May;36(4):363-9. doi: 10.1016/j.nucmedbio.2009.01.015.
Trastuzumab is a monoclonal antibody that is used in treating breast cancer. We labeled this monoclonal antibody with lutetium-177 and performed in vitro quality control tests as a first step in the production of a new radiopharmaceutical.
Trastuzumab was labeled with lutetium-177 using DOTA as chelator. Radiochemical purity and stability in buffer and human blood serum were determined using thin layer chromatography. Immunoreactivity and toxicity of the complex were tested on MCF7 breast cancer cell line.
The radiochemical purity of the complex was 96+/-0.9%. The stabilities in phosphate buffer and in human blood serum at 96 h postpreparation were 93+/-1.2% and 85+/-3.5%, respectively. The immunoreactivity of the complex was 89+/-1.4%. At a concentration of 1 nM, the complex killed 70+/-3% of MCF7 cells. At 1.9 nM, 90+/-5% of the cells were killed.
The results showed that the new complex could be considered for further evaluation in animals and possibly in humans as a new radiopharmaceutical for use in radioimmunotherapy against breast cancer.
曲妥珠单抗是一种用于治疗乳腺癌的单克隆抗体。我们用镥 - 177标记了这种单克隆抗体,并进行了体外质量控制测试,作为生产一种新型放射性药物的第一步。
使用DOTA作为螯合剂,用镥 - 177标记曲妥珠单抗。采用薄层色谱法测定其放射化学纯度以及在缓冲液和人血清中的稳定性。在MCF7乳腺癌细胞系上测试该复合物的免疫反应性和毒性。
该复合物的放射化学纯度为96±0.9%。制备后96小时,在磷酸盐缓冲液和人血清中的稳定性分别为93±1.2%和85±3.5%。该复合物的免疫反应性为89±1.4%。在浓度为1 nM时,该复合物杀死了70±3%的MCF7细胞。在1.9 nM时,90±5%的细胞被杀死。
结果表明,作为一种用于乳腺癌放射免疫治疗的新型放射性药物,这种新复合物可考虑在动物身上进一步评估,甚至可能在人体上进行评估。