Abstract
The epidermal growth factor receptor (EGFR) family includes four structurally related receptor tyrosine kinases, termed as HER1 (EGFR, erbB1), HER2 (erbB2), HER3 (erbB3), and HER4 (erbB4). Given its intimate role in the development of several solid tumors, excessive HER signaling provides a unique opportunity for anticancer intervention. Along with extensive pharmacological studies validating the therapeutic potential of targeting the EGFR family for cancer therapy, kinase inhibitors of this family are continuously coming up and entering clinical studies. Herein, we review the EGFR family small molecule kinase inhibitors which have been approved or progressed into clinical studies, mainly focusing on their mechanisms of action, structure-activity relationships, binding modes, synthetic routes, and clinical status.
Keywords: Clinical trial, EGFR/HER/erbB, small molecule inhibitor, solid tumor.
Current Medicinal Chemistry
Title:Development of EGFR Family Small Molecule Inhibitors for Anticancer Intervention: An Overview of Approved Drugs and Clinical Candidates
Volume: 21 Issue: 38
Author(s): Weiyan Cheng, Yongzhou Hu and Rong Sheng
Affiliation:
Keywords: Clinical trial, EGFR/HER/erbB, small molecule inhibitor, solid tumor.
Abstract: The epidermal growth factor receptor (EGFR) family includes four structurally related receptor tyrosine kinases, termed as HER1 (EGFR, erbB1), HER2 (erbB2), HER3 (erbB3), and HER4 (erbB4). Given its intimate role in the development of several solid tumors, excessive HER signaling provides a unique opportunity for anticancer intervention. Along with extensive pharmacological studies validating the therapeutic potential of targeting the EGFR family for cancer therapy, kinase inhibitors of this family are continuously coming up and entering clinical studies. Herein, we review the EGFR family small molecule kinase inhibitors which have been approved or progressed into clinical studies, mainly focusing on their mechanisms of action, structure-activity relationships, binding modes, synthetic routes, and clinical status.
Export Options
About this article
Cite this article as:
Cheng Weiyan, Hu Yongzhou and Sheng Rong, Development of EGFR Family Small Molecule Inhibitors for Anticancer Intervention: An Overview of Approved Drugs and Clinical Candidates, Current Medicinal Chemistry 2014; 21 (38) . https://dx.doi.org/10.2174/0929867321666140915142809
DOI https://dx.doi.org/10.2174/0929867321666140915142809 |
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
- Bentham Author Support Services (BASS)
- 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
-
The Association and Influencing Factors between Antipsychotics Exposure and the Risk of VTE and PE: A Systematic Review and Meta-analysis
Current Drug Targets Rutin as a Natural Therapy for Alzheimer's Disease: Insights into its Mechanisms of Action
Current Medicinal Chemistry Alcohol Abuse and Pancreatic Diseases: An Overview
Recent Patents on Inflammation & Allergy Drug Discovery Bisphosphonates-Anti-Inflammatory Properties
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Cell-Permeable Peptide Inhibitor of c-Jun NH2-Terminal Kinase for the Treatment of Diabetes
Current Bioactive Compounds TRYCAT Pathways Link Peripheral Inflammation, Nicotine, Somatization and Depression in the Etiology and Course of Parkinson’s Disease
CNS & Neurological Disorders - Drug Targets Estrogen: Roles in Spermatogenesis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Patent Selections
Recent Patents on DNA & Gene Sequences Role of Autophagy in Parkinson’s Disease
Current Medicinal Chemistry DNA Methylation, Chondrogenesis, and Cartilage Degeneration
Current Rheumatology Reviews Proinflammatory Cytokines in Breast Cancer: Mechanisms of Action and Potential Targets for Therapeutics
Current Drug Targets Plumbagin Inhibits Breast Tumor Bone Metastasis and Osteolysis by Modulating the Tumor-Bone Microenvironment
Current Molecular Medicine Oxidative Stress in COPD: Molecular Background and Clinical Monitoring
Current Medicinal Chemistry Pathophysiogenesis of Mesial Temporal Lobe Epilepsy: Is Prevention of Damage Antiepileptogenic?
Current Medicinal Chemistry Molecular Mechanisms of PPAR-γ Governing MSC Osteogenic and Adipogenic Differentiation
Current Stem Cell Research & Therapy Immunotherapy and Cancer Vaccines in the Management of Breast Cancer
Current Pharmaceutical Design The Impact of Inflammatory Profile on Selenium Levels in Hemodialysis Patients
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Seeing Genes at Work in the Living Brain with Non-Invasive Molecular Imaging
Current Gene Therapy Perceptions in Type 1 Diabetes Mellitus with or Without the Use of Insulin Pump: An Online Study
Current Diabetes Reviews Biology and Natural History of Type 1 Diabetes Mellitus
Current Pediatric Reviews