Original Publication Date: 30 November, 2013
Publication / Source: Lung Cancer Management
Authors: Haiying Cheng1 & Bilal Piperdi
The development of EGF receptor (EGFR) tyrosine kinase inhibitors (TKIs) has shifted our treatment paradigm in non-small-cell lung cancer (NSCLC). Erlotinib is an orally administered, first-generation, reversible EGFR TKI. The activating mutations in the tyrosine kinase domain of EGFR are considered to be the most important biomarkers to predict responses to erlotinib because these mutations are the oncologic drivers of some NSCLC by stimulating downstream signaling, such as the RAS–RAF–MEK–ERK, PI3K–AKT and STAT pathways. In the USA, erlotinib is the preferred front-line therapy in advanced EGFR-mutated NSCLC, with superior response rates and progression-free survival (PFS) in comparison to standard chemotherapy.