Second-generation epidermal growth factor tyrosine kinase inhibitors in non-small cell lung cancer

Abstract

Inhibiting the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) has an established role in the treatment of advanced non-small cell lung cancer. The first-generation EGFR inhibitors erlotinib and gefitinib have been approved for treatment in the second- and third-line setting. Second-generation EGFR tyrosine kinase inhibitors are now in development aiming to improve efficacy and overcome primary and secondary resistance to the first-generation drugs. The two most common strategies being used to achieve these aims are irreversible binding of drug to target and kinase multi-targeting. This is an overview of the early clinical development of selected second-generation tyrosine kinase inhibitors focusing on the treatment of non-small cell lung cancer.

Keywords::

• AEE788
• BIBW-2992
• CI-1033
• EGFR inhibitors
• EKB-569
• epidermal growth factor receptor
• erlotinib
• gefitinib
• HKI-272
• lapatinib
• non-small cell lung cancer
• PF-299804
• tyrosine kinase inhibitors
• vandetanib
• XL647