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Purpose: The purpose of this review article is to describe the recent data supporting the use of epidermal growth factor receptor (EGFR) receptor tyrosine kinase inhibitors (TKIs) in the first-line setting of EGFR mutation-positive non-small cell lung cancer (NSCLC). Summary: EGFR receptor TKIs were originally developed in unselected NSCLC patients and demonstrated modest clinical benefit compared to placebo. With the discovery of improved benefits in the approximately 16% of NSCLC patients with an EGFR mutation, trials in selected populations were undertaken, demonstrating comparable efficacy to standard chemotherapy with an improved toxicity profile. The most common toxicity is rash, sometimes requiring dose adjustment and discontinuation and the most serious toxicity is interstitial lung disease, which occurs in about 1% of patients treated with EGFR receptor TKIs and is fatal in 30% who develop this toxicity. CONCLUSION: The EGFR receptor TKIs are an effective therapy in EGFR-mutated NSCLC and are recommended as first-line therapy for those with advanced or metastatic disease.
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