Preclinical characterisation of 111In-DTPA-trastuzumab

摘要: Trastuzumab (Herceptin) is a recombinant humanised IgG1 monoclonal antibody against the human epidermal growth factor receptor 2 (HER2), used for metastatic breast cancer treatment. Radiolabelled trastuzumab may have several future applications diagnostic use. The aim of present study was to develop clinical grade (111)Indium ((111)In) radiolabelled trastuzumab, evaluate stability and immunoreactivity tracer perform biodistribution in tumour-bearing mice. with (111)In using DTPA as chelator. (111)In-DTPA-trastuzumab (labelling yield 92.3+/-2.3%, radiochemical purity 97.0+/-1.5%) stable PBS when stored at 4 degrees C more than 14 days. immunoreactive fraction determined by cell-binding assays, HER2-overexpressing ovarian SK-OV-3 tumour cell line, 0.87+/-0.06. Biodistribution targeting were studied HER2 receptor-positive -negative athymic HER2-positive showed (9.77+/-1.14% injected dose per gram (ID g(-1))) substantial uptake labelled already after 5 h. difference between versus tumours even pronounced 3 days injection (16.30+/-0.64% ID g(-1)), visualised radioimmunoscintigraphy. Liver, spleen kidney marked uptake. In summary, can be efficiently high labelling yields stability. selectively binds both vitro vivo animals. Therefore, appears suitable