Past studies have demonstrated that
epidermal growth factor receptor (EGFR)
tyrosine kinase inhibitors can significantly improve clinical outcomes in patients with locally advanced or metastatic
non-small cell lung cancer (NSCLC) and sensitive EGFR gene mutations.
Gefitinib (
Iressa(®)), the first oral EGFR
tyrosine kinase inhibitor, has been shown to be more effective and better tolerated than
chemotherapy either in first-line or second-line treatment for patients with advanced NSCLC harboring sensitive EGFR mutations. Conversely, among patients with wild-type EGFR,
gefitinib is inferior to standard
chemotherapy in both the first-line and second-line settings. Further,
gefitinib is effective in patients with
brain metastases because of its low molecular weight and excellent penetration of the blood-brain barrier. In this review, we summarize the current data from clinical trials with
gefitinib and appraise its role in the management of locally advanced or metastatic NSCLC.