Abstract
Lung cancer continues to be the leading cause of cancer death worldwide. Among lung cancers, 80% are classified as nonsmall- cell lung cancer (NSCLC) and are mostly diagnosed at an advanced stage (either locally advanced or metastatic disease). In the last years, the discovery of the pivotal role in tumorigenesis of the Epidermal Growth Factor Receptor (EGFR) has provided a new class of targeted therapeutic agents: the EGFR tyrosine kinase inhibitors (EGFR-TKIs). Since the first reports of an association between somatic mutations in EGFR exons 19 and 21 and response to EGFR-TKIs, treatment of advanced NSCLC has changed dramatically. Histologic profile, clinical characteristics, and mutational profile of lung carcinoma have all been reported as predictive factors of response to EGFR-TKIs and other targeted therapies. In advanced NSCLC patients harboring EGFR mutations, the use of EGFR TKIs in first-line treatment has provided an unusually large progression-free survival (PFS) benefit with a negligible toxicity when compared with cytotoxic chemotherapy in phase III randomized trials. Considering the findings regarding the excellent benefit and better safety profile of EGFR TKIs in EGFR mutation positive patients, these targeted therapeutic agents can be now considered as first-line treatment in this setting of patients. This review will discuss the new evidences in the role of EGFR-TKIs in the first-line treatment of advanced NSCLC and their implication in the current clinical decision-making.
Keywords: Acquired resistance, advanced NSCLC, epidermal growth factor mutation, erlotinib, first-line treatment, fluorescence in situ hybridization, gefitinib, immunohistochemistry, mutation detection, primary resistance, polymerase chain reaction, targeted therapy
Current Medicinal Chemistry
Title:The Role of EGFR Tyrosine Kinase Inhibitors in the First-Line Treatment of Advanced Non Small Cell Lung Cancer Patients Harboring EGFR Mutation
Volume: 19 Issue: 20
Author(s): A. Sgambato, F. Casaluce, P. Maione, A. Rossi, E. Rossi, A. Napolitano, G. Palazzolo, M. A. Bareschino, C. Schettino, P. C. Sacco, F. Ciadiello and C. Gridelli
Affiliation:
Keywords: Acquired resistance, advanced NSCLC, epidermal growth factor mutation, erlotinib, first-line treatment, fluorescence in situ hybridization, gefitinib, immunohistochemistry, mutation detection, primary resistance, polymerase chain reaction, targeted therapy
Abstract: Lung cancer continues to be the leading cause of cancer death worldwide. Among lung cancers, 80% are classified as nonsmall- cell lung cancer (NSCLC) and are mostly diagnosed at an advanced stage (either locally advanced or metastatic disease). In the last years, the discovery of the pivotal role in tumorigenesis of the Epidermal Growth Factor Receptor (EGFR) has provided a new class of targeted therapeutic agents: the EGFR tyrosine kinase inhibitors (EGFR-TKIs). Since the first reports of an association between somatic mutations in EGFR exons 19 and 21 and response to EGFR-TKIs, treatment of advanced NSCLC has changed dramatically. Histologic profile, clinical characteristics, and mutational profile of lung carcinoma have all been reported as predictive factors of response to EGFR-TKIs and other targeted therapies. In advanced NSCLC patients harboring EGFR mutations, the use of EGFR TKIs in first-line treatment has provided an unusually large progression-free survival (PFS) benefit with a negligible toxicity when compared with cytotoxic chemotherapy in phase III randomized trials. Considering the findings regarding the excellent benefit and better safety profile of EGFR TKIs in EGFR mutation positive patients, these targeted therapeutic agents can be now considered as first-line treatment in this setting of patients. This review will discuss the new evidences in the role of EGFR-TKIs in the first-line treatment of advanced NSCLC and their implication in the current clinical decision-making.
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Sgambato A., Casaluce F., Maione P., Rossi A., Rossi E., Napolitano A., Palazzolo G., A. Bareschino M., Schettino C., C. Sacco P., Ciadiello F. and Gridelli C., The Role of EGFR Tyrosine Kinase Inhibitors in the First-Line Treatment of Advanced Non Small Cell Lung Cancer Patients Harboring EGFR Mutation, Current Medicinal Chemistry 2012; 19 (20) . https://dx.doi.org/10.2174/092986712801215973
DOI https://dx.doi.org/10.2174/092986712801215973 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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