Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer

J Hill, RM Jones, D Crich - Journal of Medicinal Chemistry, 2023 - ACS Publications
Metastases to the brain remain a significant problem in lung cancer, as treatment by most
small-molecule targeted therapies is severely limited by efflux transporters at the blood …

Epidermal growth factor receptor tyrosine kinase inhibitors in the treatment of central nerve system metastases from non-small cell lung cancer

J Zhang, J Yu, X Sun, X Meng - Cancer letters, 2014 - Elsevier
Brain metastases (BM) are common and disastrous occurrence in patients with non-small
cell lung cancer (NSCLC). Currently increasing studies suggest remarkable efficacy and …

Paradigm shift of therapeutic management of brain metastases in EGFR-mutant non-small cell lung cancer in the era of targeted therapy

A Sekine, H Satoh - Medical Oncology, 2017 - Springer
Non-small cell lung cancer (NSCLC) patients with epidermal growth factor receptor (EGFR)
mutations commonly present brain metastases (BM) at the time of NSCLC diagnosis or …

The role of EGFR-TKI for leptomeningeal metastases from non-small cell lung cancer

X Yufen, S Binbin, C Wenyu, L Jialiang, Y Xinmei - Springerplus, 2016 - Springer
Leptomeningeal metastasis (LM) is a terminal event in the development of non-small cell
lung cancer (NSCLC). It has a poor prognosis with median survival of 1.9 months if …

Development of a potent brain-penetrant EGFR tyrosine kinase inhibitor against malignant brain tumors

JE Tsang, LM Urner, G Kim, K Chow… - ACS Medicinal …, 2020 - ACS Publications
The epidermal growth factor receptor (EGFR) is genetically altered in nearly 60% of
glioblastoma tumors; however, tyrosine kinase inhibitors (TKIs) against EGFR have failed to …

Gefitinib in patients with brain metastases from non–small-cell lung cancer: review of 15 clinical cases

Y Namba, T Kijima, S Yokota, M Niinaka… - Clinical lung cancer, 2004 - Elsevier
The clinical efficacy of gefitinib, a tyrosine kinase inhibitor of epidermal growth factor
receptor (EGFR), on brain metastases (BMs) from non–small-cell lung cancer (NSCLC) was …

Chemotherapy and EGFR tyrosine kinase inhibitors for treatment of brain metastases from non-small-cell lung cancer: survival analysis in 210 patients

Y Fan, Z Huang, L Fang, L Miu, N Lin… - OncoTargets and …, 2013 - Taylor & Francis
Background Chemotherapy and epidermal growth factor receptor (EGFR) tyrosine kinase
inhibitors are controversial in the treatment of patients with brain metastases from non-small …

Cerebrospinal fluid concentration of gefitinib and erlotinib in patients with non-small cell lung cancer

Y Togashi, K Masago, S Masuda, T Mizuno… - Cancer chemotherapy …, 2012 - Springer
Purpose Several cases have been reported in which central nervous system (CNS)
metastases of non-small cell lung cancer (NSCLC) resistant to gefitinib were improved by …

[HTML][HTML] Blood-brain barrier permeability of gefitinib in patients with brain metastases from non-small-cell lung cancer before and during whole brain radiation therapy

Y Zeng, H Liao, T Qin, L Zhang, W Wei, J Liang, F Xu… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Results Fifteen BM patients completed gefitinib plus WBRT. The CSF-to-plasma ratio of
gefitinib in patients with BM was higher than that in patients without BM (1.34% vs. 0.36 …

[HTML][HTML] Tyrosine Kinase Inhibitors Could Be Effective Against Non-small Cell Lung Cancer Brain Metastases Harboring Uncommon EGFR Mutations

C Ma, J Zhang, D Tang, X Ye, J Li, N Mu, Z Li… - Frontiers in …, 2020 - frontiersin.org
Background: The significance of uncommon epidermal growth factor receptor (EGFR)
mutations in patients with non-small cell lung cancer (NSCLC) and brain metastasis (BM) …