Preclinical evaluation of holmium-166 labeled anti-VEGF-A(Bevacizumab)

Radiolabeled antiangiogenic monoclonal antibodies are potential agents for targeted therapy in specific types of malignancies. In this study, 166Ho‐DOTA‐Bevacizumab was used in biodistribution studies using single‐photon emission computed tomography (SPECT) to acquire dosimetric aspects of the radio...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2013-06, Vol.56 (8), p.365-369
Main Authors: Khorami-Moghadam, Alireza, Bolouri, Bahram, Jalilian, Amir Reza, Bahrami-Samani, Nariman Mosafa, Ali, Mazidi, Seyed Mohammad, Alirezapour, Behrouz
Format: Article
Language:English
Subjects:
Angiogenesis Inhibitors - pharmacokinetics
Animals
Antibodies, Monoclonal, Humanized - pharmacokinetics
Bevacizumab
biodistribution
conjugation
Drug Evaluation, Preclinical
Holmium - pharmacokinetics
holmium-166
Mice
radiolabeling
Radiopharmaceuticals - pharmacokinetics
Rats
Tomography, Emission-Computed, Single-Photon
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Summary:Radiolabeled antiangiogenic monoclonal antibodies are potential agents for targeted therapy in specific types of malignancies. In this study, 166Ho‐DOTA‐Bevacizumab was used in biodistribution studies using single‐photon emission computed tomography (SPECT) to acquire dosimetric aspects of the radiolabeled antibody in mice. The liver toxicity of the radiolabeled antibody was also determined using serum glutamic pyruvic transaminase, serum glutamic oxaloacetic transaminase and alkaline phosphatase assay 2–7 days post‐injection. The SPECT biodistribution demonstrated a similar pattern as the other radiolabeled anti‐vascular endothelial growth factor A (VEGF‐A) immunoconjugates.166Ho‐DOTA‐Bevacizumab was revealed as a potential compound for therapy/imaging of VEGF‐A expression in oncology. Copyright © 2013 John Wiley & Sons, Ltd. 166Ho‐DOTA‐bevacizumab is a potential compound for diagnosis and treatment studies and follow‐up of VEGF expression in oncology. The uptake data for 166Ho‐DOTA‐bevacizumab is comparable with 89Zr‐bevacizumab.9. 166Ho‐DOTA‐bevacizumab imaging in wild‐type rats showed distinct accumulation of the radiotracer in the chest region after the injection.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.3044