Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance

T Zhang, R Qu, S Chan, M Lai, L Tong, F Feng, H Chen… - Molecular cancer, 2020 - Springer
cancer (NSCLC) patients with activating EGFR mutations … many other selective inhibitors
against EGFR T790M that are … caused EGFR T790M tumor shrinkage in a lung cancer patient …

EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research

RF Dong, ML Zhu, MM Liu, YT Xu, LL Yuan… - Pharmacological …, 2021 - Elsevier
EGFR downstream signalling pathways include (1) the phosphatidylinositol-3-kinase (PI3K)/protein
kinase B (AKT) pathway… (ASP8273, Astellas closed enrolment in ASP8273 studies), …

Current approaches in NSCLC targeting K-RAS and EGFR

V Aran, J Omerovic - International journal of molecular sciences, 2019 - mdpi.com
… However, promising approaches aimed to inhibit mutant K-… , the inhibition of both pathways
has led to tumour shrinkage … (AC0010), naquotinib (ASP8273) and WZ4002. They were all …

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LEL Hendriks, R Bruno - … Acquired Resistance in Lung Cancer, 2023 - books.google.com
… therapy of tumors with EGFR common activating mutations (3… SCLC patients typically achieve
tumor shrinkage with the first-… treatment with ASP8273, a Japanese 3rd G EGFR-TKI (82). …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
| Signal Transduction and Targeted Therapy … Signal Transduction and Targeted Therapy …

[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
… to be potent inhibitors of T790M-mutant EGFR, while … *, CO-1686, HM61713 and ASP8273
excluded due to halted … , 12 patients a partial response and tumour shrinkage was seen in the …

AXL confers intrinsic resistance to osimertinib and advances the emergence of tolerant cells

H Taniguchi, T Yamada, R Wang, K Tanimura… - Nature …, 2019 - nature.com
inhibition reduced the viability of EGFR-mutated lung cancer … resulted in dramatic tumor
shrinkage with the tumors never re-… with EGFR-TKIs gefitinib, erlotinib, afatinib, or ASP8273 were …

Cysteine-targeted irreversible inhibitors of tyrosine kinases and key interactions

C Hu, X Dong - Current Medicinal Chemistry, 2019 - ingentaconnect.com
… to a mutated selective EGF receptor tyrosine kinase inhibitor (TKI… -selective EGFR inhibitor
with IC50 values for EGFR(L858R )and … Phase I study suggests that ASP8273 is tolerable and …

Targeting phospholipase C using synthetic inhibitors of EGFR signaling for cancer treatment

S Krishnamoorthy, L Periyasamy, G Jayapradha… - … in Physiology and …, 2023 - Elsevier
… as ASP8273, is an irreversible EGFR inhibitor targeting … to induce tumor reduction with mutant
EGFR-positive tumors … CH7233163 is a selective inhibitor for several EGFR mutants such …

Lazertinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: results from the dose escalation and dose expansion parts of a first-in-human …

MJ Ahn, JY Han, KH Lee, SW Kim, DW Kim… - The Lancet …, 2019 - thelancet.com
EGFR tyrosine kinase inhibitors (TKIs) in patients with EGFR-mutated non-small-cell lung
cancer … response and stable disease), tumour shrinkage, and pharmacokinetics of lazertinib. …