title: Afatinib and lung cancer.
abstract: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) have an established role in the treatment of non-small-cell lung cancer (NSCLC). First-generation reversible ATP-competitive EGFR-TKIs are approved for the initial treatment of patients with EGFR mutation-positive advanced NSCLC. Afatinib is an irreversible second-generation EGFR-TKI with potent preclinical activity against EGFR (wild type and mutant), HER2, HER4 and EGFR-mutant NSCLC with acquired resistance to reversible EGFR-TKI. LUX-Lung 3 trial demonstrated superiority of afatinib to cisplatin and pemetrexed in the frontline treatment of treatment-naïve patients with advanced adenocarcinoma of the lung and EGFR mutation. Based on these results, afatinib was recently approved for the first-line treatment of NSCLC patients with EGFR mutation. This article summarizes current status of preclinical and clinical development of afatinib in NSCLC.
authors.affiliation: Department of Hospital Medicine, Cleveland Clinic, Cleveland, OH, USA.
authors.forename: Prantesh
authors.initials: P
authors.lastname: Jain
authors.forename: Rashmi
authors.initials: R
authors.lastname: Khanal
authors.forename: Aakanksha
authors.initials: A
authors.lastname: Sharma
authors.forename: Feng
authors.initials: F
authors.lastname: Yan
authors.forename: Neelesh
authors.initials: N
authors.lastname: Sharma
mesh_terms: D000077716:Afatinib; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000503:physiopathology; D002986:Clinical Trials as Topic; D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000502:physiology; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000503:physiopathology; D011799:Quinazolines / Q000627:therapeutic use*
chemical_list: D011799:Quinazolines; D000077716:Afatinib; D066246:ErbB Receptors
keywords: EGFR; NSCLC; afatinib; erlotinib; gefitinib