Preparation and in vitro evaluation of 111In-CHX-A"-DTPA-labeled anti-VEGF monoclonal antibody bevacizumab.

Bevacizumab is a humanized monoclonal antibody that binds to vascular endothelial growth factor (VEGF) and prevents tumor angiogenesis. Radionuclide imaging using radiolabeled bevacizumab might be useful for selection of patients for anti-VEGF therapy. This study describes preparation of a potential imaging agent, 111In-CHX-A"-DTPA-bevacizumab, and evaluation of specificity of its binding to three tumor cell lines, SKOV3, LS174T and DU 145. Bevacizumab was conjugated with CHX-A"-DTPA and radiolabeled with 111In with high yield and excellent stability. Specificity of cellular binding was examined by a saturation assay using 100-fold excess of non-radiolabeled antibody. SKOV3 and LS174T tumor cell lines showed significantly specific binding, while DU 145 cells did not showed any specific binding. The specific binding is dependent to type of cell lines, which it is important for selection of tumor model for scintigraphic imaging of the VEGF expression.