Developing Inhibitors of the Epidermal Growth Factor Receptor for Cancer Treatment

摘要: Progress in identifying and understanding the molecular cellular causes of cancer has led to discovery anomalies that characterize cells represent targets for development therapeutics. One such target is epidermal growth factor receptor (EGFR), a transmembrane protein frequently dysregulated cells. Preclinical studies have demonstrated pharmacologic interventions abrogate EGFR dysfunction result antitumor effects. On basis these findings, therapeutic strategies inhibit EGFR-related pathways, including use monoclonal antibodies against extracellular ligand-binding domain small-molecule inhibitors tyrosine kinase activity EGFR, entered clinical testing where they favorable safety profiles adequate pharmacology. Further agents been fueled by evidence their activities, both as single combination with chemotherapy radiation therapy. Areas require investigation are definition patient populations most likely derive benefits from drugs, implementation biologic correlative aid selection pharmacodynamically relevant doses schedules, characterization population pharmacokinetic parameters pharmacogenomic variables, appropriate scenario proceeding agents.