Radiolabeling, Characteristics and NanoSPECT/CT Imaging of 188Re-cetuximab in NCI-H292 Human Lung Cancer Xenografts

• Published in: Anticancer research Vol. 39; no. 1; pp. 183 - 190
• Main Authors: Kuo, Wan-I, Cheng, Kai-Hung, Chang, Ya-Jen, Wu, Tsung-Tse, Hsu, Wei-Chuan, Chen, Liang-Cheng, Chang, Chih-Hsien
• Format: Journal Article
• Language: English
• Published: Greece International Institute of Anticancer Research 01.01.2019
• Subjects: Binding; Cancer; Cell surface; Computed tomography; Cytotoxicity; Diagnostic software; Diagnostic systems; Epidermal growth factor receptors; Immunotherapy; Lung cancer; Medical imaging; Monoclonal antibodies; Radioisotopes; Radiolabelling; Targeted cancer therapy; Tumors; Xenografts; Xenotransplantation; cetuximab; theranostics; Rhenium-188; NCI-H292; epidermal growth factor receptor
• ISSN: 0250-7005; 1791-7530
• DOI: 10.21873/anticanres.13096

Cetuximab has exhibited high EGFR-targeting specificity and clinical promise in previous studies. In this study, we formulated unit dose kits for preparation of high specific activity Re-cetuximab for imaging and treatment of EGFR-positive cancer. Re-cetuximab was prepared by adding 0.37-0.74 GBq/0.5 ml of Re-perrhenate for 4 h at 37°C. Cell surface expression of EGFR, cell binding and cytotoxic effects were evaluated in vitro using both EGFR-positive (NCI-H292, A431) and EGFR-negative (BT483) tumors. A nanoSPECT/CT imaging study was performed in mice bearing EGFR-expressing NCI-H292 tumors. Re-cetuximab bound specifically to EGFR-expressing cells and labeling of radionuclides to cetuximab preserved the binding ability of the antibody. Besides, the cytotoxic effect of Re-cetuximab was increased dose-dependently. NanoSPECT/CT imaging revealed that Re-cetuximab could continually target the tumor region for at least 48 h. The highly specific targeted property of Re-cetuximab suggested that it is suitable as a diagnostic tool and maybe a potent radioimmunotherapy agent in EGFR-positive cancers.