Update on recent preclinical and clinical studies of T790M mutant-specific irreversible epidermal growth factor receptor tyrosine kinase inhibitors

BC Liao, CC Lin, JH Lee, JCH Yang - Journal of biomedical science, 2016 - Springer
The first-and second-generation epidermal growth factor receptor tyrosine kinase inhibitors
(1/2G EGFR-TKIs) gefitinib, erlotinib, and afatinib have all been approved as standard first …

Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

X Lu, L Yu, Z Zhang, X Ren, JB Smaill… - Medicinal research …, 2018 - Wiley Online Library
Both the first‐generation reversible epidermal growth factor receptor (EGFR) inhibitors
gefitinib and erlotinib and the second‐generation covalent epidermal growth factor receptor …

[HTML][HTML] Third-generation epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer

NMA Wright, GD Goss - Translational Lung Cancer Research, 2019 - ncbi.nlm.nih.gov
Mutations in the epidermal growth factor receptor (EGFR) gene are the most common
targetable genomic drivers of non-small cell lung cancer (NSCLC), occurring in …

[HTML][HTML] Mechanisms of resistance to irreversible epidermal growth factor receptor tyrosine kinase inhibitors and therapeutic strategies in non-small cell lung cancer

J Xu, J Wang, S Zhang - Oncotarget, 2017 - ncbi.nlm.nih.gov
Epidermal growth factor receptor (EGFR) T790M mutation is the most frequent mechanism
which accounts for about 60% of acquired resistance to first-generation EGFR tyrosine …

Efficacy of irreversible EGFR-TKIs for the uncommon secondary resistant EGFR mutations L747S, D761Y, and T854A

M Chiba, Y Togashi, E Bannno, Y Kobayashi… - BMC cancer, 2017 - Springer
Background Non-small cell lung cancer (NSCLC) harboring common epidermal growth
factor receptor (EGFR) gene mutations (exon 19 deletion or exon 21 L858R) respond to …

The EGFR T790M Mutation in Acquired Resistance to an Irreversible Second-Generation EGFR Inhibitor

Y Kim, J Ko, ZY Cui, A Abolhoda, JS Ahn, SH Ou… - Molecular cancer …, 2012 - AACR
Molecular target therapies using first-generation, reversible epidermal growth factor receptor
(EGFR) tyrosine kinase inhibitors (TKI), such as gefitinib or erlotinib, have been shown to be …

Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence

SHI Ou - Critical reviews in oncology/hematology, 2012 - Elsevier
The discovery of activating epidermal growth factor receptor (EGFR) mutations in non-small
cell lung cancer (NSCLC) in 2004 heralded the era of molecular targeted therapy in NSCLC …

Revisiting the molecular mechanism of acquired resistance to reversible tyrosine kinase inhibitors caused by EGFR gatekeeper T790M mutation in non-small-cell lung …

Y Zhao, Y Jiao, F Sun, X Liu - Medicinal Chemistry Research, 2018 - Springer
Background A variety of tyrosine kinase inhibitors (TKIs) have been developed to target
human epidermalgrowth factor receptor (EGFR) for non-small-cell lung cancer (NSCLC) …

[HTML][HTML] T790M and acquired resistance of EGFR TKI: a literature review of clinical reports

C Ma, S Wei, Y Song - Journal of thoracic disease, 2011 - ncbi.nlm.nih.gov
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) such as gefitinib
and erlotinib are promising therapies for patients with advanced non-small-cell lung cancer …

In Vitro and In Vivo Characterization of Irreversible Mutant-Selective EGFR Inhibitors That Are Wild-Type Sparing

R Tjin Tham Sjin, K Lee, AO Walter, A Dubrovskiy… - Molecular cancer …, 2014 - AACR
Patients with non–small cell lung carcinoma (NSCLC) with activating mutations in epidermal
growth factor receptor (EGFR) initially respond well to the EGFR inhibitors erlotinib and …