Original Publication Date: 17 January, 2014
Publication / Source: Lung Cancer Management
Authors: Hidetoshi Hayashi & Kazuhiko Nakagawa
In non-small-cell lung cancer (NSCLC), the discovery that EGF receptor (EGFR) signaling plays a key role in regulating cell proliferation, differentiation and tumorigenesis has emphasized the importance of targeted therapy. Small molecule tyrosine kinase inhibitors of EGFR (EGFR–TKIs), such as gefitinib and erlotinib, compete with ATP for binding to the tyrosine kinase pocket of the receptor, thereby inhibiting receptor kinase activity and EGFR signaling.