Abstract
The epidermal growth factor receptor (EGFR) is a cellular transmembrane receptor with tyrosine kinase enzymatic activity which plays a key role in human cancer. EGFR-dependent signaling is involved in cancer cell proliferation, apoptosis, angiogenesis, invasion and metastasis. Targeting the EGFR has played a central role in advancing non small cell lung cancer (NSCLC) research, treatment and patients outcome over the last several years. Two types of anti-EGFR targeting agents have reached advanced clinical development: monoclonal antibodies (Mabs) and small molecule inhibitors of the EGFR tyrosine kinase enzymatic activity (TKIs). Among TKIs gefitinib and erlotinib has been approved for the treatment of advanced NSCLC. Some clinical features such as never-smoking, female gender, East Asian origin, adenocarcinoma histology, and some biological characteristics such as somatic EGFR gene mutations and increased EGFR gene copy number, are associated with a greater benefit from treatment with TKIs. This review focuses on the clinical evidence on the anticancer activity of EGFR-TKIs in the treatmnent of NSCLC patients.
Keywords: NSCLC, EGFR pathways, Erlotinib, Gefitinib
Current Cancer Therapy Reviews
Title: Small Molecule Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Non Small Cell Lung Cancer Treatment
Volume: 3 Issue: 4
Author(s): Clorinda Schettino, Maria Anna Bareschino, Paolo Maione, Antonio Rossi, Fortunato Ciardiello and Cesare Gridelli
Affiliation:
Keywords: NSCLC, EGFR pathways, Erlotinib, Gefitinib
Abstract: The epidermal growth factor receptor (EGFR) is a cellular transmembrane receptor with tyrosine kinase enzymatic activity which plays a key role in human cancer. EGFR-dependent signaling is involved in cancer cell proliferation, apoptosis, angiogenesis, invasion and metastasis. Targeting the EGFR has played a central role in advancing non small cell lung cancer (NSCLC) research, treatment and patients outcome over the last several years. Two types of anti-EGFR targeting agents have reached advanced clinical development: monoclonal antibodies (Mabs) and small molecule inhibitors of the EGFR tyrosine kinase enzymatic activity (TKIs). Among TKIs gefitinib and erlotinib has been approved for the treatment of advanced NSCLC. Some clinical features such as never-smoking, female gender, East Asian origin, adenocarcinoma histology, and some biological characteristics such as somatic EGFR gene mutations and increased EGFR gene copy number, are associated with a greater benefit from treatment with TKIs. This review focuses on the clinical evidence on the anticancer activity of EGFR-TKIs in the treatmnent of NSCLC patients.
Export Options
About this article
Cite this article as:
Schettino Clorinda, Bareschino Anna Maria, Maione Paolo, Rossi Antonio, Ciardiello Fortunato and Gridelli Cesare, Small Molecule Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Non Small Cell Lung Cancer Treatment, Current Cancer Therapy Reviews 2007; 3 (4) . https://dx.doi.org/10.2174/157339407782496997
DOI https://dx.doi.org/10.2174/157339407782496997 |
Print ISSN 1573-3947 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6301 |
- 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
Related Articles
-
Recent Developments of Platinum-based Anticancer Drugs- Detection and Analysis in Biological Samples
Current Organic Chemistry Focal Adhesion Kinase as a Therapeutic Target of Bortezomib
Anti-Cancer Agents in Medicinal Chemistry Epothilones: A Novel Class of Non-taxane Microtubule-stabilizing Agents
Current Pharmaceutical Design ABC Transporters as Potential Targets for Modulation of Drug Resistance
Mini-Reviews in Medicinal Chemistry Future Prospect of RNA Interference for Cancer Therapies
Current Drug Targets Editorial (Hot Topic: Synthetic, Natural and Related Compounds: New Approach to Chronic Diseases Studies)
Current Topics in Medicinal Chemistry Membrane Tyrosine Kinase Receptors are an Important Target for the Therapy of Acute Myeloid Leukemia
Current Cancer Therapy Reviews Design and Synthesis of Novel Schiff Base-Benzothiazole Hybrids as Potential Epidermal Growth Factor Receptor (EGFR) Inhibitors
Anti-Cancer Agents in Medicinal Chemistry New Hopes in Cancer Battle - A Review of New Molecules and Treatment Strategies
Medicinal Chemistry Pharmacogenomics of Human ABC Transporter ABCC11 (MRP8): Potential Risk of Breast Cancer and Chemotherapy Failure
Anti-Cancer Agents in Medicinal Chemistry The Role of TNFSF15 in the Modulation of Neovascularization and Inflammation
Current Hypertension Reviews Endocannabinoid System: A Promising Therapeutic Target for the Treatment of Haematological Malignancies?
Current Medicinal Chemistry Editorial (Thematic Issue: Biosafety of Viral Vectors Commonly Used in Gene Therapy and Vaccination)
Current Gene Therapy Recent Advances in the Development of Catalytic Inhibitors of Human DNA Topoisomerase IIα As Novel Anticancer Agents
Current Medicinal Chemistry Xanthones from Mangosteen Extracts as Natural Chemopreventive Agents: Potential Anticancer Drugs
Current Molecular Medicine Pharmacological Modulation of Reactive Oxygen Species in Cancer Treatment
Current Drug Targets Regulatory Approaches to Nonclinical Reproductive Toxicity Testing of Anti-Cancer Drugs
Anti-Cancer Agents in Medicinal Chemistry Chemotherapeutic Strategies Against Trypanosoma brucei: Drug Targets vs. Drug Targeting
Current Pharmaceutical Design Clinical Development of MET Targeted Therapy For Human Cancer
Current Cancer Therapy Reviews A Systematic Review of Meta-Analyses on Gene Polymorphisms and Gastric Cancer Risk
Current Genomics