Abstract
Glioblastoma represents the most common primary brain tumor in adults. Despite improvements of multimodal therapy, the prognosis of this disease remains unfavorable. Thus, great efforts have been made to identify therapeutic agents directed against those specific molecular targets whose presence was shown to be associated with worse clinical outcomes. The epidermal growth factor receptor (HER1/EGFR) has been identified as one such target, and different compounds were developed to inhibit HER1/EGFR and/ or its mutant form, EGFRvIII. However, clinical trials did not confirm the initial enthusiasm conveyed by promising results from experimental studies. Therefore, a therapeutic approach directed at inhibiting solely HER1/EGFR does not seem to translate into a clinical benefit. This review discusses the current therapeutic situation in the setting of glioblastoma while putting the spotlight on erlotinib, a HER1/EGFR-targeted small molecule tyrosine kinase inhibitor.
Keywords: Clinical trials, combination therapy, erlotinib, glioblastoma, HER1/EGFR, small molecule tyrosine kinase inhibitors, intracellular tyrosine kinase (TK) domain, phosphatidylinositol 3-kinase (PI3-K)/Akt pathway, vascular endothelial growth factor (VEGF)
Anti-Cancer Agents in Medicinal Chemistry
Title: Erlotinib in Glioblastoma - Lost in Translation?
Volume: 11 Issue: 8
Author(s): Georg Karpel-Massler, M. Andrew Westhoff, Richard E. Kast, Christian Rainer Wirtz and Marc-Eric Halatsch
Affiliation:
Keywords: Clinical trials, combination therapy, erlotinib, glioblastoma, HER1/EGFR, small molecule tyrosine kinase inhibitors, intracellular tyrosine kinase (TK) domain, phosphatidylinositol 3-kinase (PI3-K)/Akt pathway, vascular endothelial growth factor (VEGF)
Abstract: Glioblastoma represents the most common primary brain tumor in adults. Despite improvements of multimodal therapy, the prognosis of this disease remains unfavorable. Thus, great efforts have been made to identify therapeutic agents directed against those specific molecular targets whose presence was shown to be associated with worse clinical outcomes. The epidermal growth factor receptor (HER1/EGFR) has been identified as one such target, and different compounds were developed to inhibit HER1/EGFR and/ or its mutant form, EGFRvIII. However, clinical trials did not confirm the initial enthusiasm conveyed by promising results from experimental studies. Therefore, a therapeutic approach directed at inhibiting solely HER1/EGFR does not seem to translate into a clinical benefit. This review discusses the current therapeutic situation in the setting of glioblastoma while putting the spotlight on erlotinib, a HER1/EGFR-targeted small molecule tyrosine kinase inhibitor.
Export Options
About this article
Cite this article as:
Karpel-Massler Georg, Andrew Westhoff M., E. Kast Richard, Rainer Wirtz Christian and Halatsch Marc-Eric, Erlotinib in Glioblastoma - Lost in Translation?, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (8) . https://dx.doi.org/10.2174/187152011797378788
DOI https://dx.doi.org/10.2174/187152011797378788 |
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
-
Role of Monocarboxylate Transporters in Drug Delivery to the Brain
Current Pharmaceutical Design Nanoliposome is a Promising Carrier of Protein and Peptide Biomolecule for the Treatment of Cancer
Anti-Cancer Agents in Medicinal Chemistry Receptor for AGEs (RAGE) as Mediator of NF-kB Pathway Activation in Neuroinflammation and Oxidative Stress
CNS & Neurological Disorders - Drug Targets Polo-Like Kinases (Plks) are Prognostic Markers for Gynecologic Malignancies
Current Women`s Health Reviews Patent Selections
Recent Patents on Anti-Cancer Drug Discovery Feasibility of Targeting Glioblastoma Stem Cells: From Concept to Clinical Trials
Current Topics in Medicinal Chemistry Naturally-occurring Dimers of Flavonoids as Anticarcinogens
Anti-Cancer Agents in Medicinal Chemistry Synergistic Effect of α-Solanine and Cisplatin Induces Apoptosis and Enhances Cell Cycle Arrest in Human Hepatocellular Carcinoma Cells
Anti-Cancer Agents in Medicinal Chemistry Alkaloids as Important Scaffolds in Therapeutic Drugs for the Treatments of Cancer, Tuberculosis, and Smoking Cessation
Current Topics in Medicinal Chemistry Anti-Genes: siRNA, Ribozymes and Antisense
Current Pharmaceutical Biotechnology Targeting Glioblastoma Stem Cells: Cell Surface Markers
Current Medicinal Chemistry A Review on Chitosan in Drug Delivery for Treatment of Neurological and Psychiatric Disorders
Current Pharmaceutical Biotechnology Synthesis of (R)-2-benzylmorpholine employing catalytic stereospecific rearrangement of L-Phenylalaninol
Letters in Organic Chemistry In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH<sub>2</sub>Ph)]Br
Anti-Cancer Agents in Medicinal Chemistry Interfering with Hedgehog Pathway: New Avenues for Targeted Therapy in Rhabdomyosarcoma
Current Drug Targets The Smart Targeting of Nanoparticles
Current Pharmaceutical Design PEDF as an Emerging Therapeutic Candidate for Osteosarcoma
Current Cancer Drug Targets MicroRNAs as Regulators in Normal Hematopoietic and Leukemia Stem Cells: Current Concepts and Clinical Implications
Current Molecular Medicine Immunophilin Dysfunction and Neuropathology
Current Medicinal Chemistry The Effectiveness of Nanoparticles on Gene Therapy for Glioblastoma Cells Apoptosis: A Systematic Review
Current Gene Therapy