Whole-exome sequencing identifies key mutated genes in T790M wildtype/cMET-unamplified lung adenocarcinoma with acquired resistance to first-generation EGFR tyrosine kinase inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Cancer Research and Clinical Oncology"
DOI: 10.1007/s00432-018-2634-4
Abstract: PurposeLung cancer is the leading cause of cancer-related death worldwide. Lung adenocarcinoma harboring EGFR-activating mutations will inevitably acquire resistance to first-generation EGFR tyrosine kinase inhibitors (TKIs). EGFR T790M mutation and cMET amplification are common mechanisms.… read more here.
Keywords: lung adenocarcinoma; first generation; generation egfr; resistance first ... See more keywords
Third generation EGFR TKIs in EGFR-mutated NSCLC: Where are we now and where are we going.
Sign Up to like & getrecommendations! Published in 2017 at "Critical reviews in oncology/hematology"
DOI: 10.1016/j.critrevonc.2017.07.003
Abstract: The therapeutic landscape of Non Small Lung Cancer (NSCLC) has been profoundly changed over the last decade with the clinical introduction of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) and the discovery of… read more here.
Keywords: generation egfr; egfr mutated; egfr; egfr tkis ... See more keywords
Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma.
Sign Up to like & getrecommendations! Published in 2021 at "Drug discovery today"
DOI: 10.1016/j.drudis.2021.02.005
Abstract: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are preferred treatments for non-small cell lung carcinoma (NSCLC) that have EGFR activating mutations. Although the initial responses to first- to third-generation EGFR-TKIs is impressive, these agents… read more here.
Keywords: generation egfr; egfr; egfr inhibitors; non small ... See more keywords
Diverse EGFR Exon 20 Insertions and Co‐Occurring Molecular Alterations Identified by Comprehensive Genomic Profiling of NSCLC
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DOI: 10.1016/j.jtho.2018.06.019
Abstract: Introduction: EGFR exon 20 insertions (EGFRex20ins) comprise an uncommon subset of EGFR‐activating alterations relatively insensitive to first‐ and second‐generation EGFR tyrosine kinase inhibitors (TKIs). However, recent early clinical data suggests these patients may benefit from… read more here.
Keywords: generation egfr; egfr; comprehensive genomic; egfr exon ... See more keywords
Design, Synthesis, and Evaluation of (R)-8-((Tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as Novel Selective ACK1 Inhibitors to Combat Acquired Resistance to the Third-Generation EGFR Inhibitor.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00319
Abstract: Activated Cdc42-associated kinase 1 (ACK1) alterations have been considered to mediate bypass acquired resistance to the third-generation EGFR inhibitors (ASK120067 and osimertinib) in NSCLC. Despite many efforts to develop ACK1 small molecule inhibitors, no selective… read more here.
Keywords: acquired resistance; resistance third; tetrahydrofuran methyl; third generation ... See more keywords
Osimertinib and other third-generation EGFR TKI in EGFR-mutant NSCLC patients
Sign Up to like & getrecommendations! Published in 2018 at "Annals of Oncology"
DOI: 10.1093/annonc/mdx704
Abstract: Osimertinib was the first third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) to receive FDA and EMA approval for metastatic EGFR-mutant non-small-cell lung cancer (NSCLC) patients that have acquired the EGFR T790M resistance… read more here.
Keywords: generation egfr; nsclc patients; egfr mutant; third generation ... See more keywords
Transformation of NSCLC to SCLC after 1st- and 3rd-generation EGFR-TKI resistance and response to EP regimen and erlotinib
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DOI: 10.1097/md.0000000000025046
Abstract: Abstract Rationale: Genotypic and histological evolution of non-small-cell lung cancer (NSCLC) into small-cell lung cancer (SCLC) has been described as a mechanism of acquired resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)… read more here.
Keywords: generation egfr; case treated; resistance; egfr ... See more keywords
Detection and monitoring of driver mutations by next‐generation sequencing in squamous cell lung cancer patient and possible predictive biomarker of third generation EGFR‐tyrosine kinase inhibitors
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DOI: 10.1111/1759-7714.12551
Abstract: Driver mutation detection and the development of targeted drugs have significantly improved survival of advanced lung adenocarcinoma patients with driver mutations. However, we still lack understanding of druggable mutations in patients with advanced squamous cell… read more here.
Keywords: generation egfr; squamous cell; generation; cancer ... See more keywords
Abstract 73: Inhibition of ACK1 delays and overcomes acquired resistance of EGFR mutant NSCLC cells to the third generation EGFR inhibitor, osimertinib
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DOI: 10.1158/1538-7445.am2019-73
Abstract: The approval of osimertinib (AZD9291) as a third generation EGFR inhibitor for treating non-small cell lung cancer (NSCLC) patients with activating EGFR mutations (first-line) or those who have become resistant to 1st generation EGFR inhibitors… read more here.
Keywords: generation egfr; egfr mutant; resistance; acquired resistance ... See more keywords
Abstract 4005: PH009-1, a highly potent and selective fourth-generation EGFR-TKI overcoming EGFR common mutations and T790M/C797S-mediated resistance in NSCLC
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4005
Abstract: Background: Epidermal growth factor receptor (EGFR) activating mutations have been reported in 10-50% of patients with non-small cell lung cancer (NSCLC). The common mutations, ex19del (D) and L858R (L) substitution, are sensitive to first- and… read more here.
Keywords: common mutations; egfr tki; c797s; generation egfr ... See more keywords
Abstract CT066: HERTHENA-Lung02: A randomized Phase 3 study of patritumab deruxtecan vs platinum-based chemotherapy in locally advanced or metastatic EGFR-mutated NSCLC after progression with a third-generation EGFR tyrosine kinase inhibitor
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-ct066
Abstract: Background: Standard therapies for patients with epidermal growth factor receptor-mutated (EGFRm) non-small cell lung cancer (NSCLC) that has progressed after treatment with third-generation EGFR tyrosine kinase inhibitors (TKIs) offer only limited benefit. Human epidermal growth… read more here.
Keywords: third generation; progression; generation egfr; egfr tki ... See more keywords