Abstract
The epidermal growth factor receptor (EGFR) is a cellular transmembrane receptor with tyrosine kinase enzymatic activity which plays a key role in human cancer. EGFR-dependent signaling is involved in cancer cell proliferation, apoptosis, angiogenesis, invasion and metastasis. Targeting the EGFR has played a central role in advancing non small cell lung cancer (NSCLC) research, treatment and patients outcome over the last several years. Two types of anti-EGFR targeting agents have reached advanced clinical development: monoclonal antibodies (Mabs) and small molecule inhibitors of the EGFR tyrosine kinase enzymatic activity (TKIs). Among TKIs gefitinib and erlotinib has been approved for the treatment of advanced NSCLC. Some clinical features such as never-smoking, female gender, East Asian origin, adenocarcinoma histology, and some biological characteristics such as somatic EGFR gene mutations and increased EGFR gene copy number, are associated with a greater benefit from treatment with TKIs. This review focuses on the clinical evidence on the anticancer activity of EGFR-TKIs in the treatmnent of NSCLC patients.
Keywords: NSCLC, EGFR pathways, Erlotinib, Gefitinib
Current Cancer Therapy Reviews
Title: Small Molecule Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Non Small Cell Lung Cancer Treatment
Volume: 3 Issue: 4
Author(s): Clorinda Schettino, Maria Anna Bareschino, Paolo Maione, Antonio Rossi, Fortunato Ciardiello and Cesare Gridelli
Affiliation:
Keywords: NSCLC, EGFR pathways, Erlotinib, Gefitinib
Abstract: The epidermal growth factor receptor (EGFR) is a cellular transmembrane receptor with tyrosine kinase enzymatic activity which plays a key role in human cancer. EGFR-dependent signaling is involved in cancer cell proliferation, apoptosis, angiogenesis, invasion and metastasis. Targeting the EGFR has played a central role in advancing non small cell lung cancer (NSCLC) research, treatment and patients outcome over the last several years. Two types of anti-EGFR targeting agents have reached advanced clinical development: monoclonal antibodies (Mabs) and small molecule inhibitors of the EGFR tyrosine kinase enzymatic activity (TKIs). Among TKIs gefitinib and erlotinib has been approved for the treatment of advanced NSCLC. Some clinical features such as never-smoking, female gender, East Asian origin, adenocarcinoma histology, and some biological characteristics such as somatic EGFR gene mutations and increased EGFR gene copy number, are associated with a greater benefit from treatment with TKIs. This review focuses on the clinical evidence on the anticancer activity of EGFR-TKIs in the treatmnent of NSCLC patients.
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Schettino Clorinda, Bareschino Anna Maria, Maione Paolo, Rossi Antonio, Ciardiello Fortunato and Gridelli Cesare, Small Molecule Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Non Small Cell Lung Cancer Treatment, Current Cancer Therapy Reviews 2007; 3 (4) . https://dx.doi.org/10.2174/157339407782496997
DOI https://dx.doi.org/10.2174/157339407782496997 |
Print ISSN 1573-3947 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6301 |
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argeted Protein Degradation is gaining momentum in cancer therapy, it facilitate targeting undruggable proteins, it overcome cancer resistance and avoid undesirable side effects. Thus small molecules degraders have emerged as novel therapeutic strategy. Targeted protein degradation (TPD), the process of eliminating a protein of interest hold a great promise for ...read more
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