[HTML][HTML] Mechanisms of resistance to EGFR-targeted drugs: lung cancer

F Morgillo, CM Della Corte, M Fasano, F Ciardiello - ESMO open, 2016 - Elsevier
Despite the improvement in clinical outcomes derived by the introduction of epidermal
growth factor receptor (EGFR) tyrosine kinase inhibitors (EGFR-TKIs) in the treatment of …

Osimertinib for pretreated EGFR Thr790Met-positive advanced non-small-cell lung cancer (AURA2): a multicentre, open-label, single-arm, phase 2 study

G Goss, CM Tsai, FA Shepherd, L Bazhenova… - The lancet …, 2016 - thelancet.com
Background Osimertinib (AZD9291) is an oral, potent, irreversible EGFR tyrosine-kinase
inhibitor selective for EGFR tyrosine-kinase inhibitor sensitising mutations, and the EGFR …

Plasma EGFR T790M ctDNA status is associated with clinical outcome in advanced NSCLC patients with acquired EGFR-TKI resistance

D Zheng, X Ye, MZ Zhang, Y Sun, JY Wang, J Ni… - Scientific reports, 2016 - nature.com
Abstract EGFR T790M mutation occurs in half of non-small cell lung cancer (NSCLC)
patients with acquired EGFR-TKI (TKI) resistance, based on tumor re-biopsies using an …

[HTML][HTML] The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients

SG Wu, YN Liu, MF Tsai, YL Chang, CJ Yu, PC Yang… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Results Forty-two patients had tissue specimens taken after acquiring resistance to afatinib.
The sensitizing EGFR mutation were all consistent between pre-and post-afatinib tissues …

First-line erlotinib therapy until and beyond response evaluation criteria in solid tumors progression in Asian patients with epidermal growth factor receptor mutation …

K Park, CJ Yu, SW Kim, MC Lin, V Sriuranpong… - JAMA …, 2016 - jamanetwork.com
Importance Continuing molecularly targeted treatment beyond disease progression in non–
small-cell lung cancer (NSCLC) has appeared promising in retrospective analyses …

Circulating tumor DNA identified by targeted sequencing in advanced-stage non-small cell lung cancer patients

S Xu, F Lou, Y Wu, DQ Sun, JB Zhang, W Chen, H Ye… - Cancer letters, 2016 - Elsevier
Non-small cell lung cancers (NSCLC) have unique mutation patterns, and some of these
mutations may be used to predict prognosis or guide patient treatment. Mutation profiling …

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 …

Osimertinib Western and Asian clinical pharmacokinetics in patients and healthy volunteers: implications for formulation, dose, and dosing frequency in pivotal clinical …

D Planchard, KH Brown, DW Kim, SW Kim… - Cancer Chemotherapy …, 2016 - Springer
Abstract Purpose Osimertinib (AZD9291) 80 mg once daily is approved by the US FDA for
the treatment of patients with metastatic EGFR T790M-positive NSCLC whose disease has …

Circulating tumor DNA detection in lung cancer patients before and after surgery

N Guo, F Lou, Y Ma, J Li, B Yang, W Chen, H Ye… - Scientific reports, 2016 - nature.com
Circulating tumor DNA (ctDNA) in peripheral blood is a “liquid biopsy” that contains
representative tumor information including gene mutations. Additionally, repeated ctDNA …

Metabolic disposition of osimertinib in rats, dogs, and humans: insights into a drug designed to bind covalently to a cysteine residue of epidermal growth factor …

PA Dickinson, MV Cantarini, J Collier, P Frewer… - Drug Metabolism and …, 2016 - ASPET
Preclinical and clinical studies were conducted to determine the metabolism and
pharmacokinetics of osimertinib and key metabolites AZ5104 and AZ7550. Osimertinib was …