Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

Pao, William; Chmielecki, Juliann

doi:10.1038/nrc2947

Cited by 1,083Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchCancer Genomics and Diagnostics

Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

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Pao, William, Chmielecki, Juliann·2010·Nature Reviews Cancer

DOI 10.1038/nrc2947PMC PMC3072803

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Abstract

Epidermal growth factor receptor (EGFR)-mutant non-small-cell lung cancer (NSCLC) was first recognized in 2004 as a distinct, clinically relevant molecular subset of lung cancer. The disease has been the subject of intensive research at both the basic scientific and clinical levels, becoming a paradigm for how to understand and treat oncogene-driven carcinomas. Although patients with EGFR-mutant tumours have increased sensitivity to tyrosine kinase inhibitors (TKIs), primary and acquired resistance to these agents remains a major clinical problem. This Review summarizes recent developments aimed at treating and ultimately curing the disease.

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The third-generation drug retains the acrylamide group and covalently binds to Cys797, but replaces the quinazoline portion of the first- and second-generation compounds with pyrimidine to promote selectivity for T790M, showing a higher affinity for T790M than WT-EGFR.
“The third-generation drug retains the acrylamide group and covalently binds to Cys797, but replaces the quinazoline portion of the first- and second-generation compounds with pyrimidine to promote selectivity for T790M, showing a higher affinity for T790M than WT-EGFR.119”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [119]
EGFR mutations occur in 10-35% of NSCLC and confer sensitivity to erlotinib, gefitinib, and afatinib.
“Mutations in EGFR occur in 10-35% of NSCLCs and confer sensitivity to the EGFR TKIs erlotinib, gefitinib, and afatinib (6).”
From AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer (2014) · cites this paper as [6]
Exon 20 insertion mutations make up 4-10% of all EGFR mutations in NSCLC.
“Exon 20 insertion mutations comprise 4–10% of all EGFR mutations 27,29–32.”
From Structural, Biochemical, and Clinical Characterization of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations in Lung Cancer (2013) · cites this paper as [30]
ERBB2 amplification and gain-of-function EGFR mutations support proliferation of various cancer cell types.
“Indeed, while ERBB2 gene amplifications and gain-of-function EGFR mutations support the proliferation of various cancer cell types (Oh and Bang, 2020; Pao and Chmielecki, 2010), VEGFA is critical for tumor-driven neoangiogenesis (Apte et al., 2019) and TGFb promotes the establishment of a fibrotic microenvironment that is poorly permissive to access by therapeutics (Derynck et al., 2020).”
From Immunomodulation by targeted anticancer agents (2021) · cites this paper as Pao and Chmielecki, 2010
HER2-, EGFR-, and VEGFA-specific agents have been licensed for various oncological indications.
“Over the past two decades, a number of mAbs and TKIs have been developed to target these proteins or their binding partners, and some of these molecules, including HER2-, EGFR-, and VEGFA-specific agents, have been licensed for use in a variety of oncological indications (Apte et al., 2019; Oh and Bang, 2020; Pao and Chmielecki, 2010).”
From Immunomodulation by targeted anticancer agents (2021) · cites this paper as Pao and Chmielecki, 2010

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Bronchial and Peripheral Murine Lung Carcinomas Induced by T790M-L858R Mutant EGFR Respond to HKI-272 and Rapamycin Combination Therapy
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An integrated genomic analysis of lung cancer reveals loss of DUSP4 in EGFR-mutant tumors
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Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.
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High dose weekly erlotinib achieves therapeutic concentrations in CSF and is effective in leptomeningeal metastases from epidermal growth factor receptor mutant lung cancer
Clarke, J. L., Pao, W., Wu, N., Miller, V. A., & Lassman, A. B. (2010) · Journal of Neuro-Oncology · doi:10.1007/s11060-010-0128-6 · Cited by 214 · see citing works
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The T790M “gatekeeper” mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor
Godin-Heymann, N., Ulkus, L., Brannigan, B. W., McDermott, U., Lamb, J. A., Maheswaran, S., Settleman, J. E., & Haber, D. A. (2008) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-07-2387 · Cited by 206 · see citing works
Alterations in Genes of the EGFR Signaling Pathway and Their Relationship to EGFR Tyrosine Kinase Inhibitor Sensitivity in Lung Cancer Cell Lines
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Analysis of epidermal growth factor receptor expression as a predictive factor for response to gefitinib (‘Iressa’, ZD1839) in non-small-cell lung cancer
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Bypassing cellular EGF receptor dependence through epithelial-to-mesenchymal-like transitions
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Emergence of Epidermal Growth Factor Receptor T790M Mutation during Chronic Exposure to Gefitinib in a Non–Small Cell Lung Cancer Cell Line
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Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib
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Epidermal Growth Factor Receptor Mutations in Small Cell Lung Cancer
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Phase II Trial of Cetuximab in Patients With Previously Treated Non–Small-Cell Lung Cancer
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ZD6474 – a novel inhibitor of VEGFR and EGFR tyrosine kinase activity
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Effects of Erlotinib in EGFR Mutated Non-Small Cell Lung Cancers with Resistance to Gefitinib
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Epithelial-mesenchymal transition in EGFR-TKI acquired resistant lung adenocarcinoma.
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Proapoptotic BH3-Only BCL-2 Family Protein BIM Connects Death Signaling from Epidermal Growth Factor Receptor Inhibition to the Mitochondrion
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Oncogenic Activity of Epidermal Growth Factor Receptor Kinase Mutant Alleles Is Enhanced by the T790M Drug Resistance Mutation
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Nodular fasciitis, a lesion of myofibroblasts.An ultrastructural study
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Mect1-Maml2 fusion oncogene linked to the aberrant activation of cyclic AMP/CREB regulated genes.
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High Expression Levels of Total IGF-1R and Sensitivity of NSCLC Cells In Vitro to an Anti-IGF-1R Antibody (R1507)
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Differential Responses to Erlotinib in Epidermal Growth Factor Receptor (EGFR)-Mutated Lung Cancers With Acquired Resistance to Gefitinib Carrying the L747S or T790M Secondary Mutations
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Sequential occurrence of non-small cell and small cell lung cancer with the same EGFR mutation
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Evolution of Resistance to Targeted Anti-Cancer Therapies during Continuous and Pulsed Administration Strategies
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Effect of re-treatment with gefitinib (‘Iressa’, ZD1839) after acquisition of resistance
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EGFR-T790M Is a Rare Lung Cancer Susceptibility Allele with Enhanced Kinase Activity
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The phosphatase and tensin homolog regulates epidermal growth factor receptor (EGFR) inhibitor response by targeting EGFR for degradation
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Mucoepidermoid carcinoma of lung: Potential target of EGFR-directed treatment
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Retreatment of Lung Adenocarcinoma Patients With Gefitinib Who Had Experienced Favorable Results From Their Initial Treatment With This Selective Epidermal Growth Factor Receptor Inhibitor: A Report of Three Cases
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CI-1033, an irreversible pan-erbB receptor inhibitor and its potential application for the treatment of breast cancer
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Analysis of Genetic Variants in Never-Smokers with Lung Cancer Facilitated by an Internet-Based Blood Collection Protocol: A Preliminary Report
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The Insulin-Like Growth Factor Pathway in Lung Cancer
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Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations
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Erlotinib resistance in mouse models of epidermal growth factor receptor-induced lung adenocarcinoma
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Erlotinib at a Dose of 25 mg Daily for Non-small Cell Lung Cancers with EGFR Mutations
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Double EGFR mutants containing rare EGFR mutant types show reduced in vitro response to gefitinib compared with common activating missense mutations
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Preliminary activity and safety results from a phase I clinical trial of PF-00299804, an irreversible pan-HER inhibitor, in patients (pts) with NSCLC
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Gefitinib as targeted therapy for mucoepidermoid carcinoma of the lung: Possible significance of CRTC1–MAML2 oncogene
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Germ-Line and Somatic Presentations of the EGFR T790M Mutation in Lung Cancer
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Epidermal growth factor receptor tyrosine kinase inhibitors as first-line treatment in advanced nonsmall-cell lung cancer
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Differences underlying EGFR and HER2 oncogene addiction
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Living With Imperfection
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Chemotherapy of Advanced Non-Small Cell Lung Cancer
Pirker, R., & Minar, W. (2009) · Frontiers of radiation therapy and oncology · doi:10.1159/000262471 · Cited by 17 · see citing works
Molecular On/Off Switch
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Mechanisms and strategies on drug resistance of EGFR-mutant non-small cell lung cancer
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Authors: Pao, W., & Chmielecki, J.
Affiliations: Vanderbilt University (US)
Corresponding author: Pao, William
ORCID: Pao, William
Chmielecki, Juliann
Venue: Nature Reviews Cancer
Publisher: Springer Science and Business Media LLC
Published: 2010-10-22
Volume: 10
Issue: 11
Pages: 760-774
ISSN: 1474-175X (ISSN-L)
1474-1768
DOI: 10.1038/nrc2947
PMC: PMC3072803
OpenAlex: W2090029719
Cited by: 1,083
References: 180
Citations by year: 2026: 24 · 2025: 43 · 2024: 54 · 2023: 49 · 2022: 45 · 2021: 65 · 2020: 79 · 2019: 56 · 2018: 69 · 2017: 72 · 2016: 90 · 2015: 82 · 2014: 93 · 2013: 93 · 2012: 104
FWCI: 14.65
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.springer.com/tdm (tdm)
Locations: Nature reviews. Cancer (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: Vanderbilt University
National Institutes of Health
University of California, San Francisco
National Cancer Institute (P30 CA 68485, R01CA121210, P01CA129243, CA90949, U54CA143798, P50CA090949, P30CA068485)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Genomics and Diagnostics
Keywords: EGFR-mutant non-small cell lung cancer, epidermal growth factor receptor, tyrosine kinase inhibitors, gefitinib, erlotinib, acquired drug resistance, primary resistance, targeted therapy
MeSH terms: Antineoplastic Agents, Carcinoma, Non-Small-Cell Lung, Humans, Lung Neoplasms, Mutation, Protein-Tyrosine Kinases, Drug Resistance, Neoplasm, Protein Kinase Inhibitors, ErbB Receptors

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Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

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