![conference banner](/images/conference-banner.jpeg)
Abstract
Specific and reversible EGFR tyrosine kinase inhibitors (TKI) such as gefitinib and erlotinib are clinically active in advanced or metastatic NSCLC and both are approved in various countries for the treatment of patients that failed prior chemotherapy. Erlotinib has also prolonged survival in pancreatic cancer patients when added to gemcitabine and regulatory approval in this disease is being sought. Additional promising activity has been seen in other tumor types, such as ovarian cancer or head and neck malignancies, and phase III trials in these malignancies are ongoing or planned. Despite these successes, these agents have exhibited anecdotal or modest activity when used as single agents in unselected patients with various other tumor types. We have learned that the clinical development of these agents is far from simple and we need to better understand biological and clinical criteria for patient selection and how to best use the different available agents. The recent discovery of EGFR mutations and the potential identification of other markers that might predict patient response could help to optimize the use of these agents in the future. Irreversible EGFR inhibitors, dual EGF/HER2 and pan-ErbB receptor inhibitors may have greater antitumor activity although the tolerance of these compounds compared to specific EGFR TKIs needs further characterization. HER2 specific TKIs are also in development. Lapatinib, a dual EGFR/HER2 TK inhibitors, is particularly promising in breast cancer. Newer agents, such as BMS-599626, have recently entered into the clinic .In addition to the use of these agents as single agents, many clinical studies are addressing the role of combining them with hormonal agents, biological agents or chemotherapy.
Keywords: egfr, her2, gefitinib, erlotinib, lapatinib, nsclc, breast cancer
Current Drug Targets
Title: Small Molecules with EGFR-TK Inhibitor Activity
Volume: 6 Issue: 3
Author(s): Joan Albanell and Pere Gascon
Affiliation:
Keywords: egfr, her2, gefitinib, erlotinib, lapatinib, nsclc, breast cancer
Abstract: Specific and reversible EGFR tyrosine kinase inhibitors (TKI) such as gefitinib and erlotinib are clinically active in advanced or metastatic NSCLC and both are approved in various countries for the treatment of patients that failed prior chemotherapy. Erlotinib has also prolonged survival in pancreatic cancer patients when added to gemcitabine and regulatory approval in this disease is being sought. Additional promising activity has been seen in other tumor types, such as ovarian cancer or head and neck malignancies, and phase III trials in these malignancies are ongoing or planned. Despite these successes, these agents have exhibited anecdotal or modest activity when used as single agents in unselected patients with various other tumor types. We have learned that the clinical development of these agents is far from simple and we need to better understand biological and clinical criteria for patient selection and how to best use the different available agents. The recent discovery of EGFR mutations and the potential identification of other markers that might predict patient response could help to optimize the use of these agents in the future. Irreversible EGFR inhibitors, dual EGF/HER2 and pan-ErbB receptor inhibitors may have greater antitumor activity although the tolerance of these compounds compared to specific EGFR TKIs needs further characterization. HER2 specific TKIs are also in development. Lapatinib, a dual EGFR/HER2 TK inhibitors, is particularly promising in breast cancer. Newer agents, such as BMS-599626, have recently entered into the clinic .In addition to the use of these agents as single agents, many clinical studies are addressing the role of combining them with hormonal agents, biological agents or chemotherapy.
Export Options
About this article
Cite this article as:
Albanell Joan and Gascon Pere, Small Molecules with EGFR-TK Inhibitor Activity, Current Drug Targets 2005; 6 (3) . https://dx.doi.org/10.2174/1389450053765888
DOI https://dx.doi.org/10.2174/1389450053765888 |
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
RNA Molecules in the Treatment of Human Diseases
Messenger and non-coding RNAs, including long and small transcripts, are mediators of gene expression. Gene expression at the RNA level shows significant aberrations in human diseases, including cancer, leukemia, lymphoma, cardiovascular diseases, and neurological disorders. Human transcripts serve either as biomarkers of diagnosis, prognosis, prediction of treatment response, and/or therapy ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Bridging ‘Green’ with Nanoparticles: Biosynthesis Approaches for Cancer Management and Targeting of Cancer Stem Cells
Current Nanoscience Ribozyme- and Deoxyribozyme-Strategies for Medical Applications
Current Drug Targets Thrombospondins as Anti-Angiogenic Therapeutic Agents
Current Pharmaceutical Design Effects of Amine Oxidases in Allergic and Histamine-Mediated Conditions
Recent Patents on Inflammation & Allergy Drug Discovery Role of Mitochondrial Heat-shock Proteins and Immunophilins in Neuro Degenerative Diseases
Current Drug Targets Phytocannabinoids and Cannabimimetic Drugs: Recent Patents in Central Nervous System Disorders
Recent Patents on CNS Drug Discovery (Discontinued) Carbon Nanotubes: An Emerging Drug Delivery Carrier in Cancer Therapeutics
Current Drug Delivery Novel Mitotic Targets and Their Small-Molecule Inhibitors
Current Cancer Drug Targets Hepatocellular Carcinoma Detection by Gallium Scan and Subsequent Treatment by Gallium Maltolate: Rationale and Case Study
Anti-Cancer Agents in Medicinal Chemistry Supramolecular Chiro-Biomedical Assays and Enantioselective HPLC Analyses for Evaluation of Profens as Non-Steroidal Anti-Inflammatory Drugs, Potential Anticancer Agents and Common Xenobiotics
Current Drug Discovery Technologies From Adipose Tissue Protein Secretion to Adipopharmacology of Disease
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Scutellarin Suppressed Proliferation and Induced Apoptosis in Gastric Cancer via Wnt/β-catenin Signaling Pathway
Current Pharmaceutical Design Cancer Stem Cells in Prostate Cancer Chemoresistance
Current Cancer Drug Targets Evidence of Probiotics in Prevention of Allergy and Asthma
Current Drug Targets - Inflammation & Allergy Therapeutic Potential of Melatonin in the Regulation of MiR-148a-3p and Angiogenic Factors in Breast Cancer
MicroRNA A Common Biological Mechanism in Cancer and Alzheimers Disease?
Current Alzheimer Research Retinoids in Clinical Use
Medicinal Chemistry Bioinformatics Approach for Data Capturing: The Case of Breast Cancer
Current Cancer Therapy Reviews Isoproterenol-induced Upregulation of HPSE Accelerates Triple-negative Breast Cancer Cell Proliferation and Migration through Enhancing the Transcriptional Activity of HIF-1α
Anti-Cancer Agents in Medicinal Chemistry Cytotoxicity and Toxicity to Animals and Humans of Ribosome-Inactivating Proteins
Mini-Reviews in Medicinal Chemistry