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.
Export Options
About this article
Cite this article as:
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 |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the Treatment of Chronic Inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Prognostic Impact of Tissue Inhibitor of Metalloproteinase-1 in Non- Small Cell Lung Cancer: Systematic Review and Meta-Analysis
Current Medicinal Chemistry New Targets, New Agents, and the Evolving Phenomena of Drug Resistance in Cancer
Current Cancer Therapy Reviews Nonviral Vectors for Cancer Gene Therapy: Prospects for Integrating Vectors and Combination Therapies
Current Gene Therapy Understanding XPO1 Target Networks Using Systems Biology and Mathematical Modeling
Current Pharmaceutical Design Development of Anti-HIV Agents Targeting Dynamic Supramolecular Mechanism: Entry and Fusion Inhibitors Based on CXCR4/CCR5 Antagonists and gp41-C34-Remodeling Peptides
Current HIV Research Incorporation of Targeted Agents in the Management of Patients with Advanced Gastric Cancer
Current Medicinal Chemistry Soft Matter Assemblies as Nanomedicine Platforms for Cancer Chemotherapy: A Journey from Market Products Towards Novel Approaches
Current Topics in Medicinal Chemistry Cisplatin Is a DNA-Damaging Antitumour Compound Triggering Multifactorial Biochemical Responses in Cancer Cells: Importance of Apoptotic Pathways
Current Medicinal Chemistry - Anti-Cancer Agents Recent Anticancer Cytotoxic Agents
Current Medicinal Chemistry - Anti-Cancer Agents Recent Advances in Positron Emission Tomography (PET) Imaging of Biomolecules: From Chemical Labeling to Cancer Diagnostics
Mini-Reviews in Organic Chemistry Reactive Oxygen Species, Cancer and Anti-Cancer Therapies
Current Chemical Biology Comparative Proteomics and Bioinformatics Analysis of Tissue from Non-Small Cell Lung Cancer Patients
Current Proteomics Promising Activity of Mammalian Target of Rapamycin Inhibitors in Hematologic Malignancies Therapy
Current Signal Transduction Therapy Irreversible Inhibition of Serine Proteases – Design and In Vivo Activity of Diaryl α-Aminophosphonate Derivatives
Current Medicinal Chemistry Pharmacokinetics and Pharmacodynamics of Lipidic Nano-Particles in Cancer
Anti-Cancer Agents in Medicinal Chemistry The Endeavours in RAS Inhibition - the Past, Present, and Future
Current Topics in Medicinal Chemistry Stage N2/IIIA Non Small Cell Lung Cancer: An Evidence-Based Review
Current Cancer Therapy Reviews In silico Studies Toward the Discovery of Novel Type-II Inhibitors of TrkA: Pharmacophore-based 3D-QSAR Modeling, Database Screening and Molecular Docking
Letters in Drug Design & Discovery Subcellular Detection and Localization of the Drug Transporter P-Glycoprotein in Cultured Tumor Cells
Current Protein & Peptide Science Arsenic-exposed Keratinocytes Exhibit Differential microRNAs Expression Profile; Potential Implication of miR-21, miR-200a and miR-141 in Melanoma Pathway
Clinical Cancer Drugs