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The Role of EGFR-TKIs in the 
Management of NSCLC

Herbert H Loong MBBS, MRCP1, Tony S Mok MD, FRCP(C)1,2

Lung cancer is the leading cause of cancer-related mortality, and accounted for >1.3 million deaths worldwide in 2007 [1]. Approximately 85% of patients with lung cancer have NSCLC, which is commonly subtyped into squamous cell carcinoma, adenocarcinoma, large cell carcinoma, and not-otherwise-specified (NOS) histologies. The majority of patients with NSCLC present with advanced stage disease [2], and the current standard therapy is a platinum-based doublet combination including a third-generation cytotoxic chemotherapy [3]. Trials comparing different platinum-based combinations have, in general, revealed similar efficacy and differing toxicity profiles [4]. However, novel targeted therapies that interfere with specific molecular signaling pathways have also emerged as a standard option for selected patients. Recent prospective and retrospective studies have validated the efficacy of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in patients with advanced NSCLC who have mutations in EGFR. Furthermore, there are clinical characteristics that predict the incidence of mutations in EGFR. The objectives of this review are to examine the current role, optimal use, and future developmental directions of EGFR-TKIs in the changing landscape of NSCLC management.

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