Abstract
Antiangiogenic monoclonal antibodies in combination with therapeutic radionuclides are potential targeted therapy agents in cancer. In this study, bevacizumab was successively labeled with [166Ho]HoCl3 after conjugation with DOTA-NHS-ester with a radiochemical purity of higher than 95% (RTLC). The conjugates were purified by molecular filtration, the average number of DOTA conjugated per mAb was calculated and total concentration was determined by spectrophotometric method and the average chelate to antibody ratio (c/a) for the conjugate used in this study was 5.8:1 and protein integrity experiments (SDS-PAGE). The biodistribution studies in wild-type rats demonstrate a similar pattern to the other radiolabeled anti-vascular endothelial growth factor A (VEGF-A) immunoconjugates. 166Ho-DOTA-bevacizumab is a potential compound for therapy/imaging of VEGF-A expression in oncology.
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