Critical Appraisal of Gefitinib in the Treatment of Non-Small Cell Lung Cancer

The leading cause of death from malignant tumors worldwide is lung cancer. Before the development of molecularly targeted therapy, chemotherapy with platinum-based doublets was considered as the standard first-line treatment in advanced non-small cell lung cancer (NSCLC) patients. The introduction of epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) has led to remarkable advances in the treatment of NSCLC. Two activating EGFR mutations (Exon 19 deletion and Exon 21 L858R mutation) have been correlated with dramatic responses to EGFR-TKI. Every effort should be made to identify the EGFR mutation status in NSCLC patients prior to the initial systemic treatment in order to select those who are most likely to benefit from EGFR-TKIs. At the present time, first-generation EGFR-TKIs are available for clinical use, including gefitinib and erlotinib. Gefitinib was the first drug developed as an EGFR-TKI for NSCLC treatment. Several randomized phase III studies revealed that gefitinib provided superior response rate, improved PFS, and less toxicity compared with doublet chemotherapy for advanced NSCLC with activating EGFR mutation. Currently, first-line treatment with gefitinib is used in metastatic NSCLC patients with tumor EGFR mutation. Gefitinib is also administered as salvage therapy for NSCLC patients previously treated with chemotherapy. The standard of care for previously untreated patients with EGFR mutation-negative or unknown status still remains platinum-based chemotherapy. In this article, we have reviewed the relevant clinical data regarding gefitinib as a molecularly targeted therapy for NSCLC.