期刊
EXPERT OPINION ON INVESTIGATIONAL DRUGS
卷 18, 期 3, 页码 293-301出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543780902762843
关键词
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
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.
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