Epidermal growth factor receptor mutations, small-molecule kinase inhibitors, and non-small-cell lung cancer: current knowledge and future directions.

Abstract excerpt

PURPOSE: Gefitinib and erlotinib are small molecules that selectively inhibit epidermal growth factor receptor (EGFR) tyrosine kinase activity. When these drugs were introduced into the clinic, the specific targets affected in human tumors were unknown. In April 2004, two groups reported that mutations in the tyrosine kinase domain of EGFR are strongly associated with gefitinib sensitivity in patients with...

Topics

• Carcinoma, Non-Small-Cell Lung
• Clinical Trials as Topic
• DNA Mutational Analysis
• ErbB Receptors
• Erlotinib Hydrochloride
• Gefitinib
• Gene Amplification
• Humans
• Lung Neoplasms
• Mutation