EGFR-Directed Monoclonal Antibodies

“Targeted therapy” designates a new generation of antitumor agents designed to interfere with a specific molecular target believed to have a critical role in tumor growth or progression. Most of these targets are represented by kinases controlling cell homeostasis, such as tyrosine kinase receptors (TKRs). The epidermal growth factor receptor (EGFR) is one of the most investigated TKRs frequently expressed in a variety of epithelial tumors and correlates with poor prognosis. Several efforts have been made in the last 20 years to design therapeutic agents that inhibit EGFR, such as monoclonal antibodies (MAbs) or tyrosine kinase inhibitors (TKIs). Cetuximab is the first anti-EGFR monoclonal antibody approved by the FDA for the treatment of patients with EGFR-expressing, metastatic colorectal carcinoma, and head and neck cancer. Other MAbs directed against EGFR, including panitumumab, are in clinical development for the treatment of various human cancer types.