67Ga-CHX-A"-DTPA-(anti-EGFR) radioimmunoconjugate as a potential agent for radioimmunoscintigraphy: Production, quality control and preclinical evaluation

Document Type : Original Article

Authors

1 Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, Iran

2 Pars Isotope Company, Tehran, IRAN

Abstract

Colorectal cancer radioimmunoscintigraphy targeting the EGFR (epidermal growth factor receptor) protein is a growing field in nuclear molecular medicine research. In this study, the average number of the chelator coupled to cetuximab was estimated in different molar excess of chelator added to conjugation reaction (50, 80, 120), the data revealed that the average number of CHX-A"-DTPA coupled to mAb was estimated to be 4.1 ± 0.49 c/a in subsequently 50 molar excess of chelator added to the conjugation reaction, then conjugated mAb with high binding affinity to the target protein was labeled with 67GaCl3 with high percentage of radiochemical purity (>98%). In vitro stability of the monoclonal antibody in phosphate buffer and human blood serum was determined using thin layer chromatography, which indicated a radiochemical purity more than 97% and 91% after 48 h, respectively. The high binding affinity of labeled Cetuximab to the target protein was obtained by determining radioimmunoreactivity and its internalization using the human colorectal adenocarcinoma SW480 cells and CHO, an epithelial cell line generated from the ovary of the Chinese hamster, (control) which showed a high binding affinity around 83%. The 67Ga-DTPA-(anti-EGFR) radioimmunoconjugate is a potential compound for SPECT molecular imaging for diagnosis and also for other therapeutic studies in oncology.

Keywords

References

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