Second-Generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers Journal Article
| Authors: | Yu, H. A.; Riely, G. J. |
| Article Title: | Second-Generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers |
| Abstract: | EGFR mutations identify patients who are more likely to respond to treatment with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) than cytotoxic chemotherapy. The distinct success of the first-generation EGFR TKIs erlotinib and gefitinib has been accompanied by the observation that acquired resistance to these treatments develops after a median of 1 year of treatment. Newer, second-generation EGFR TKIs have been developed with the intent to delay or overcome acquired resistance by the broader inhibition of kinases (eg, HER2 and vascular endothelial growth factor receptor) and/or altering the interactions with EGFR through irreversibly binding to the kinase domain. This article discusses many of these agents (including afatinib, dacomitinib, XL647, AP26113, and CO-1686) which have the potential for greater efficacy compared with first-generation EGFR TKIs, and may also have clinical activity against other oncogenic mutations within the EGFR family, including HER2. Copyright © 2013 JNCCN-Journal of the National Comprehensive Cancer Network. |
| Keywords: | cancer chemotherapy; unclassified drug; mutation; erlotinib; advanced cancer; antineoplastic agents; clinical trials as topic; vasculotropin receptor; enzyme inhibition; lung non small cell cancer; lung neoplasms; epidermal growth factor receptor; epidermal growth factor receptor 2; randomized controlled trials as topic; receptor, epidermal growth factor; drug resistance, neoplasm; protein kinase inhibitors; gefitinib; vandetanib; epidermal growth factor receptor kinase inhibitor; neratinib; xl 647; afatinib; dacomitinib; bms 690514; ap 26113; co 1686 |
| Journal Title: | Journal of the National Comprehensive Cancer Network |
| Volume: | 11 |
| Issue: | 2 |
| ISSN: | 1540-1405 |
| Publisher: | Harborside Press |
| Date Published: | 2013-02-01 |
| Start Page: | 161 |
| End Page: | 169 |
| Language: | English |
| PROVIDER: | scopus |
| PUBMED: | 23411383 |
| PMCID: | PMC3673302 |
| DOI/URL: | |
| Notes: | --- - "Export Date: 1 April 2013" - "Source: Scopus" |
