BAY 2927088: The first non-covalent, potent, and selective tyrosine kinase inhibitor targeting EGFR exon 20 insertions and C797S resistance mutations in NSCLC

被引：0

作者：

Siegel, F. ^{[1
]}

Siegel, S. ^{[2
]}

Graham, K. ^{[3
]}

Karsli-Uzunbas, G. ^{[4
]}

Korr, D. ^{[5
]}

Schroeder, J. ^{[5
]}

Boemer, U. ^{[6
]}

Hillig, R. C. ^{[7
]}

Mortier, J. ^{[8
]}

Niehues, M. ^{[9
]}

Golfier, S. ^{[10
]}

Schulze, V. ^{[2
]}

Menz, S. ^{[11
]}

Kamburov, A. ^{[12
]}

Hermsen, M. ^{[13
]}

Cherniak, A. ^{[4
]}

Eis, K. ^{[4
,14
]}

Eheim, A. ^{[1
]}

Meyerson, M. ^{[15
]}

Greulich, H. ^{[4
]}

机构：

[1] Bayer, Res & Early Development Precis Mol Oncol, Cambridge, MA USA

[2] Bayer, Drug Discovery Sci, Berlin, Germany

[3] Boehringer Ingelheim GmbH & Co KG, Med Chem, Berlin, Germany

[4] Broad Inst & Harvard, Canc Program, Cambridge, MA USA

[5] Nuvisan, Therapeut Res, Berlin, Germany

[6] Nuvisan, Biochem, Berlin, Germany

[7] Nuvisan, Struct Biol, Berlin, Germany

[8] Bayer, Computat Chem, Berlin, Germany

[9] Nuvisan, Struct & Sample Analyt, Berlin, Germany

[10] Nuvisan, Translat Res, Berlin, Germany

[11] Bayer, DMPK Modeling & Simulat, Berlin, Germany

[12] Bayer, Biomed Data Sci, Berlin, Germany

[13] Inst Invest Sanitaria Principado Asturias ISPA, Dept Head & Neck Canc, Oviedo, Spain

[14] Bayer, Drug Discovery Sci, Cambridge, MA USA

[15] Dana Farber Canc Ctr, Ctr Canc Genome Discovery, Boston, MA USA

来源：

EUROPEAN JOURNAL OF CANCER | 2022年 / 174卷

关键词：

D O I：

暂无

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

引用

页码：S9 / S10

页数：2

共 27 条

[21] PH009-1, a highly potent and selective fourth-generation EGFR-TKI overcoming EGFR common mutations and T790M/C797S-mediated resistance in NSCLC
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[22] AZD9291: an irreversible, potent and selective third generation tyrosine kinase inhibitor (TKI) targeting EGFR activating (EGFRm plus ) and resistance (T790M) mutations in advanced lung adenocarcinoma.
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[23] BLU-701 is a highly potent, brain-penetrant and WT-sparing next-generation EGFR TKI for the treatment of sensitizing (ex19del, L858R) and C797S resistance mutations in metastatic NSCLC.
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[24] BREED based de novo hybridization approach: generating novel T790M/C797S-EGFR tyrosine kinase inhibitors to overcome the problem of mutation and resistance in non small cell lung cancer (NSCLC)
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[25] Computational and Synthetic approach with Biological Evaluation of Substituted Quinoline derivatives as small molecule L858R/T790M/C797S triple mutant EGFR inhibitors targeting resistance in Non-Small Cell Lung Cancer (NSCLC)
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[26] Free energy perturbation guided Synthesis with Biological Evaluation of Substituted Quinoline derivatives as small molecule L858R/T790M/C797S mutant EGFR inhibitors targeting resistance in Non-Small Cell Lung Cancer (NSCLC)
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[27] Primary Resistance to Combination Therapy with First- and Third-Generation EGFR Tyrosine Kinase Inhibitors of Lung Adenocarcinoma Harboring EGFR 19Del/T790M/in Trans-C797S Mutations with Co-Occurring CTNNB1 Alteration
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Wu, Xilin
ONCOTARGETS AND THERAPY, 2020, 13 : 6749 - 6753

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