Abstract
Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) have changed the paradigm of treatment in non-small cell lung cancer (NSCLC). The molecular biology study of EGFR has led to clinical trials that select patients more accurately, regarding the presence of EGFR activating mutations. Nonetheless, a lack of response or a temporary condition of the response has been detected in patients on EGFR TKIs. This has urged to study potential resistance mechanisms underneath. The most important ones are the presence of secondary mutations in EGFR, such as T790M, or the overexpression of mesenchymal-epithelial transition factor (MET) that may explain why patients who initially respond to EGFR TKIs, may ultimately become refractory. Several approaches have been taken and new drugs both targeting EGFR resistance-mutation or MET are currently being developed. Here we review and update the EGFR biological pathway as well as the clinical data leading to approval of the EGFR TKIs currently in the market. New compounds under investigation targeting resistance mutations or dually targeting EGFR and other relevant receptors are also reviewed and discussed.
Keywords: Activity mutations, epidermal growth factor receptor, tyrosine kinase inhibitors.
Current Drug Targets
Title:Epidermal Growth Factor Receptor Targeting in Non-Small Cell Lung Cancer: Revisiting Different Strategies Against the Same Target
Volume: 15 Issue: 14
Author(s): Eduardo Castanon, Patricia Martin, Christian Rolfo, Juan P. Fusco, Lucia Ceniceros, Jairo Legaspi, Marta Santisteban and Ignacio Gil-Bazo
Affiliation:
Keywords: Activity mutations, epidermal growth factor receptor, tyrosine kinase inhibitors.
Abstract: Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) have changed the paradigm of treatment in non-small cell lung cancer (NSCLC). The molecular biology study of EGFR has led to clinical trials that select patients more accurately, regarding the presence of EGFR activating mutations. Nonetheless, a lack of response or a temporary condition of the response has been detected in patients on EGFR TKIs. This has urged to study potential resistance mechanisms underneath. The most important ones are the presence of secondary mutations in EGFR, such as T790M, or the overexpression of mesenchymal-epithelial transition factor (MET) that may explain why patients who initially respond to EGFR TKIs, may ultimately become refractory. Several approaches have been taken and new drugs both targeting EGFR resistance-mutation or MET are currently being developed. Here we review and update the EGFR biological pathway as well as the clinical data leading to approval of the EGFR TKIs currently in the market. New compounds under investigation targeting resistance mutations or dually targeting EGFR and other relevant receptors are also reviewed and discussed.
Export Options
About this article
Cite this article as:
Castanon Eduardo, Martin Patricia, Rolfo Christian, Fusco P. Juan, Ceniceros Lucia, Legaspi Jairo, Santisteban Marta and Gil-Bazo Ignacio, Epidermal Growth Factor Receptor Targeting in Non-Small Cell Lung Cancer: Revisiting Different Strategies Against the Same Target, Current Drug Targets 2014; 15 (14) . https://dx.doi.org/10.2174/138945011514141216092935
DOI https://dx.doi.org/10.2174/138945011514141216092935 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
Drug-Targeted Approach with Polymer Nanocomposites for Improved Therapeutics
Polymer nanocomposites have been recognized as an advanced and cutting-edge technique in drug targeting administration. These materials combine the unique features of nanoparticles with the adaptability of polymers to produce highly personalized drug administration devices. Integrating nanoparticles containing pharmaceuticals into a polymer matrix enables researchers to regulate the rates at ...read more
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...read more
Therapeutic Chemical and RNA Design with Artificial Intelligence
Computer-Aided Drug Design (CADD) has emerged as a fundamental component of modern drug discovery. Molecular docking facilitates virtual screening on a large scale through structural simulations. However, traditional CADD approaches face significant limitations, as they can only screen known compounds from existing libraries. PubChem, as the most widely used chemical ...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
Related Articles
-
Novel Lipid and Polymeric Materials as Delivery Systems for Nucleic Acid Based Drugs
Current Drug Metabolism Implementing Cancer Exercise Rehabilitation: An Update on Recommendations for Clinical Practice
Current Cancer Therapy Reviews Aspirin: A Potential Therapeutic Approach in Pancreatic Cancer
Current Medicinal Chemistry Small Players With Big Roles: MicroRNAs as Targets to Inhibit Breast Cancer Progression
Current Drug Targets MicroRNAs and Targeted Therapies in Non-small Cell Lung Cancer: Minireview
Anti-Cancer Agents in Medicinal Chemistry 18F-Labeled Proteins
Current Pharmaceutical Biotechnology Mitochondria-Targeting Anticancer Metal Complexes
Current Medicinal Chemistry Cytotoxicity of Novel Sulfanilamides Towards Sensitive and Multidrugresistant Leukemia Cells
Current Medicinal Chemistry Bradykinin Antagonists as Anti-Cancer Agents
Current Pharmaceutical Design Design, Synthesis and Anticancer Activity Evaluation of Diazepinomicin Derivatives
Letters in Drug Design & Discovery Safety Profiles and Pharmacovigilance Considerations for Recently Patented Anticancer Drugs: Advanced Thyroid Cancer
Recent Patents on Anti-Cancer Drug Discovery The De Novo Synthesis of Oligosaccharides: Application to the Medicinal Chemistry SAR-Study of Digitoxin
Current Topics in Medicinal Chemistry α(N)-Heterocyclic Thiosemicarbazones: Iron Chelators that are Promising for Revival of Gallium in Cancer Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry Sulfur-Containing Compounds in Protecting Against Oxidant-Mediated Lung Diseases
Current Medicinal Chemistry Current Development of ROS-Modulating Agents as Novel Antitumor Therapy
Current Cancer Drug Targets HLA Class I Expression, Tumor Escape and Cancer Progression
Current Cancer Therapy Reviews Cytotoxicity and Cell Death Mechanisms Induced by a Novel Bisnaphthalimidopropyl Derivative against the NCI-H460 non-small Lung Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry Biological Strategies to Enhance Rotator Cuff Healing.
Current Stem Cell Research & Therapy Phase II and Pharmacological Study of Oral Docetaxel Plus Cyclosporin A in Anthracycline Pre-Treated Metastatic Breast Cancer
Current Clinical Pharmacology Bisacylimidoselenocarbamates Cause G2/M Arrest Associated with the Modulation of CDK1 and Chk2 in Human Breast Cancer MCF-7 Cells
Current Medicinal Chemistry