Abstract
Amplification of the HER2/neu gene occurs in approximately 20-25% of invasive breast cancers and is associated with poor patient outcome. The development of trastuzumab, a humanized monoclonal antibody that binds to the extracellular domain of HER2, has led to a significant improvement in outcomes of patients with HER2-positive breast cancer. However, many patients with HER2- positive metastatic breast cancer do not respond to trastuzumab, or eventually become resistant to it. In addition, approximately 15% of patients treated with trastuzumab-based therapy in the adjuvant setting relapse. In this review, we discuss the mechanisms of antitumor activity of trastuzumab, potential mechanisms contributing to its resistance, and novel therapeutic agents that may provide a means to overcome trastuzumab resistance.
Anti-Cancer Agents in Medicinal Chemistry
Title: Mechanisms of Trastuzumab Resistance in Breast Cancer
Volume: 9 Issue: 3
Author(s): Sara M. Tolaney and Ian E. Krop
Affiliation:
Abstract: Amplification of the HER2/neu gene occurs in approximately 20-25% of invasive breast cancers and is associated with poor patient outcome. The development of trastuzumab, a humanized monoclonal antibody that binds to the extracellular domain of HER2, has led to a significant improvement in outcomes of patients with HER2-positive breast cancer. However, many patients with HER2- positive metastatic breast cancer do not respond to trastuzumab, or eventually become resistant to it. In addition, approximately 15% of patients treated with trastuzumab-based therapy in the adjuvant setting relapse. In this review, we discuss the mechanisms of antitumor activity of trastuzumab, potential mechanisms contributing to its resistance, and novel therapeutic agents that may provide a means to overcome trastuzumab resistance.
Export Options
About this article
Cite this article as:
Tolaney M. Sara and Krop E. Ian, Mechanisms of Trastuzumab Resistance in Breast Cancer, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (3) . https://dx.doi.org/10.2174/1871520610909030348
DOI https://dx.doi.org/10.2174/1871520610909030348 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Therapeutic Approaches Using Riboflavin in Mitochondrial Energy Metabolism Disorders
Current Drug Targets Synthesis and Pharmacological Evaluation of Maleopimaric N-arylimides: Identification of Novel Proapoptotic Agents
Anti-Cancer Agents in Medicinal Chemistry Genetic Polymorphisms of Drug Metabolizing Enzymes and Transporters: The Long Way from Bench to Bedside
Current Topics in Medicinal Chemistry Synthesis and In Vitro Cytotoxic Activity Evaluation of Novel Mannich Bases and Modified AZT Derivatives Possessing Mannich Base Moieties via Click Chemistry
Letters in Drug Design & Discovery Cardiac Fat as New Diagnostic Tool and Potential Therapeutic Target for Obesity Management and Treatment
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Effects of Estrogen in the Brain: Is it a Neuroprotective Agent in Alzheimers Disease?
Current Aging Science Linc01638 Promotes Tumorigenesis in HER2+ Breast Cancer
Current Cancer Drug Targets Multidrug Resistance in Cancer Chemotherapy and Xenobiotic Protection Mediated by the Half ATP-Binding Cassette Transporter ABCG2
Current Medicinal Chemistry - Anti-Cancer Agents P-Glycoprotein - Implications of Metabolism of Neoplastic Cells and Cancer Therapy
Current Cancer Drug Targets Novel Targets for Antiinflammatory and Antiarthritic Agents
Current Pharmaceutical Design The Role of Mediterranean Diet, CoQ10 and Conjugated-Melatonin in Osteoporosis Primary Prevention and Therapy
Current Nutrition & Food Science Exploring the use of Estrogen & Progesterone Replacement Therapy in Subarachnoid Hemorrhage
Current Drug Safety Raman Spectroscopy-based Metabonomics of HIV-infected Sera Detects Amino Acid and Glutathione Changes
Current Metabolomics EGFR and EML4-ALK Updated Therapies in Non-Small Cell Lung Cancer
Recent Patents on Anti-Cancer Drug Discovery Solid Lipid Nanoparticles: A Potential Approach for Drug Delivery System
Nanoscience & Nanotechnology-Asia Psychosocial Stress, Emotions and Cytokine-Related Disorders
Recent Patents on Inflammation & Allergy Drug Discovery Serial Analysis of Gene Expression in Eukaryotic Pathogens
Infectious Disorders - Drug Targets The Role of Emerging Genomics and Proteomics Technologies in Cancer Drug Target Discovery
Current Cancer Drug Targets Editorial [Hot Topic: Ulcerative Colitis: A Cinderella Story (Guest Editor: Silvio Danese)]
Current Drug Targets Chemical and Radiochemical Considerations in Radiolabeling with α-Emitting Radionuclides
Current Radiopharmaceuticals