Afatinib and lung cancer

作者：Jain Prantesh; Kh**** Rashmi; Sharma Aakanksha; Yan Feng; Sharma Neelesh^*

来源：Expert Review of Anticancer Therapy, 2014, 14(12): 1391-1406.

DOI：10.1586/14737140.2014.983083

• afatinib
• EGFR
• erlotinib
• gefitinib
• NSCLC

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-naive 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.

• 出版日期2014-12