New acrylamide-substituted quinazoline derivatives with enhanced potency for the treatment of EGFR T790M-mutant non-small-cell lung cancers.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.01.035
Abstract: A new class of acrylamide-substituted quinazoline derivatives with enhanced inhibitory activity against mutant EGFR T790M enzyme were synthesized. Among them, compound 10b displayed the strongest inhibitory potency to block the phosphorylation of the EGFR T790M… read more here.
Keywords: egfr; compound 10b; egfr t790m; t790m ... See more keywords
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFRL858R/T790M inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.11.069
Abstract: Third-generation epidermal growth factor receptor (EGFR)L858R/T790M inhibitors are still the main drugs for the treatment of advanced non-small cell lung cancer (NSCLC), and these drugs have achieved remarkable clinical efficacy. However, there are still many… read more here.
Keywords: design synthesis; t790m inhibitors; t790m; egfrl858r t790m ... See more keywords
Most T790M mutations are present on the same EGFR allele as activating mutations in patients with non-small cell lung cancer.
Sign Up to like & getrecommendations! Published in 2017 at "Lung cancer"
DOI: 10.1016/j.lungcan.2017.02.019
Abstract: OBJECTIVES The T790M and C797S mutations of the epidermal growth factor receptor gene (EGFR) confer resistance to first- and third-generation EGFR tyrosine kinase inhibitors (TKIs), respectively, in patients with non-small cell lung cancer (NSCLC) harboring… read more here.
Keywords: cell; lung cancer; activating mutations; t790m ... See more keywords
Developing Ultrasensitive Library-Aliquot-Based Droplet Digital PCR for Detecting T790M in Plasma-Circulating Tumor DNA of Non-small-Cell-Lung-Cancer Patients.
Sign Up to like & getrecommendations! Published in 2018 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.8b01776
Abstract: A T790M secondary mutation in epidermal-growth-factor receptor (EGFR) is the most well-established EGFR-tyrosine-kinase-inhibitor (TKI) resistance marker in non-small-cell lung cancer (NSCLC). The current methods to rapidly and accurately detect T790M in clinical practice are not… read more here.
Keywords: tumor; lab ddpcr; dna; t790m ... See more keywords
Strategien zur Überwindung der erworbenen EGFR-TKI-Resistenz durch T790M spezifische Substanzen am Beispiel von Osimertinib
Sign Up to like & getrecommendations! Published in 2018 at "Pneumologie"
DOI: 10.1055/a-0647-9835
Abstract: Die Resistenzbildung gegenüber der 1. und 2. Generation von Tyrosinkinase-Inhibitoren (TKIs) des epidermalen Wachstumsfaktors (EGFR) stellt bei der Behandlung von Patienten mit nicht kleinzelligem Lungenkarzinom, die eine aktivierende Mutation im EGFR aufweisen, ein großes Problem dar.… read more here.
Keywords: bei; von; egfr tkis; t790m ... See more keywords
Differential efficacy of Osimertinib in EGFR T790M positive non-small cell lung cancer by metastatic site
Sign Up to like & getrecommendations! Published in 2019 at "Annals of Oncology"
DOI: 10.1093/annonc/mdz338.080
Abstract: Abstract Background Osimertinib is a standard treatment for non-small cell lung cancer(NSCLC) with common and T790M EGFR mutation and efficacy for brain metastasis is reported. However there are only a few reports regarding efficacy or… read more here.
Keywords: t790m; metastasis; efficacy; non small ... See more keywords
Osimertinib for compound EGFR exon 19 deletion/T790M mutated lung squamous cell carcinoma
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DOI: 10.1111/1759-7714.13431
Abstract: The role of the epidermal growth factor receptor (EGFR) mutation status testing in lung squamous cell carcinoma (SqCC) remains controversial. Evidence of the effectiveness of osimertinib in SqCC with EGFR T790M mutation is limited. Here,… read more here.
Keywords: egfr exon; cell carcinoma; squamous cell; t790m ... See more keywords
T790M-Selective EGFR-TKI Combined with Dasatinib as an Optimal Strategy for Overcoming EGFR-TKI Resistance in T790M-Positive Non–Small Cell Lung Cancer
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-17-0351
Abstract: T790M mutation–selective EGFR tyrosine kinase inhibitors (EGFR-TKI) have demonstrated clinical benefits in non–small cell lung cancer (NSCLC) patients harboring T790M mutation, which is the major cause of resistance to EGFR-TKI. However, their efficacy is limited,… read more here.
Keywords: t790m positive; selective egfr; egfr tki; t790m ... See more keywords
Abstract LB-B03: Exosome-based Detection of EGFR T790M in Plasma from Non-Small Cell Lung Cancer Patients
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-17-lb-b03
Abstract: About 60% of non-small cell lung cancer (NSCLC) patients develop resistance to targeted epidermal growth factor receptor (EGFR) inhibitor therapy through the EGFR T790M mutation. Although these patients respond well to third generation tyrosine kinase… read more here.
Keywords: egfr; detection; plasma; t790m ... See more keywords
Abstract 4016: Discovery of a small-molecule EGFR inhibitor that can potently target various EGFR mutants, including C797S mutant, in vitro and in vivo
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4016
Abstract: EGFR is one of receptor tyrosine kinases (RTKs) and, upon ligand binding, turns on the downstream signals that include oncogenic RAS/MEK/ERK, PI3K/AKT/mTOR, and JAK/STAT pathways. EGFR gene mutations, such as Exon 19 deletion (Del19) and… read more here.
Keywords: small molecule; egfr mutants; inhibitor; t790m ... See more keywords
Abstract B32: RADIANCE: An open-label, nonrandomized, prospective biomarker study to assess analytic concordance between noninvasive testing and tissue testing for EGFR T790M mutation detection in patients with non-small cell lung cancer
Sign Up to like & getrecommendations! Published in 2018 at "Clinical Trials"
DOI: 10.1158/1557-3265.aacriaslc18-b32
Abstract: Background: EGFR-TKIs are the recommended first-line therapy of patients (pts) with advanced non-small cell lung cancer (NSCLC) who have an EGFR-sensitizing mutation (EGFRm). However, most pts develop resistance to EGFR-TKIs, with the EGFR T790M resistance… read more here.
Keywords: egfr; detection; t790m; tissue ... See more keywords