Anti-hEGFR-hIgG2 features the constant region of the human IgG2 isotype and the variable region of cetuximab. Cetuximab is a chimeric human/mouse IgG1 monoclonal antibody that targets EGFR, a cell surface receptor overexpressed in many types of cancer. EGFR is activated by binding specific ligands, including epidermal growth factor and transforming growth factor-α.
Activation of EGFR promotes cell proliferation and survival, as well as angiogenesis, leading to tumor growth and metastasis. Binding of cetuximab to EGFR blocks ligand‑receptor binding and induces receptor internalization and subsequent degradation. Consequently, cetuximab blocks downstream pathways which regulate cell growth and angiogenesis. In addition, cetuximab induces cell death through antibody-dependent cell-mediated cytotoxicity (ADCC) [1,2].
Cetuximab has been approved by the FDA for the treatment of metastatic colorectal cancer and metastatic squamous cell carcinoma of the head and neck .
Anti-hEGFR-hIgG2 was generated by recombinant DNA technology. It has been produced in CHO cells and purified by affinity chromatography with protein G.
- Kurai J. et al., 2007. Antibody-dependent cellular cytotoxicity mediated by cetuximab against lung cancer cell lines. Clin Cancer Res. 3(5):1552-61.
- Kimura H. et al., 2007. Antibody-dependent cellular cytotoxicity of cetuximab against tumor cells with wild-type or mutant epidermal growth factor receptor. Cancer Sci. 98(8):1275-80.
- Vincenzi B. et al., 2010. Cetuximab: from bench to bedside. Curr Cancer Drug Targets. 10(1):80-95.