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

[1] Chronicles of EGFR Tyrosine Kinase Inhibitors: Targeting EGFR C797S Containing Triple Mutations
Duggirala, Krishna Babu
Lee, Yujin
Lee, Kwangho
BIOMOLECULES & THERAPEUTICS, 2022, 30 (01) : 19 - 27
[2] Mechanisms of resistance to BAY 2927088, the first reversible inhibitor targeting EGFR exon 20 insertion mutations in non-small cell lung cancer
Uzunbas, Gizem Karsli
McVeigh, Quinn
Gupta, Akansha
Hoyt, Stephanie
Doucette, Kristen
Keshishian, Hasmik
Carr, Steven
Yang, Xiaoping
Root, David
Cherniack, Andrew D.
Siegel, Franziska
Siegel, Stephan
Meyerson, Matthew
Greulich, Heidi
MOLECULAR CANCER THERAPEUTICS, 2023, 22 (12)
[3] Mechanisms of resistance to BAY 2927088, the first reversible inhibitor targeting EGFR exon 20 insertion mutations in non-small cell lung cancer
Uzunbas, Gizem Karsli
McVeigh, Quinn
Gupta, Akansha
Hoyt, Stephanie
Cherniack, Andrew
Siegel, Franziska
Siegel, Stephan
Meyerson, Matthew
Greulich, Heidi
CANCER RESEARCH, 2023, 83 (07)
[4] The EGFR C797S Mutation Confers Resistance to a Novel EGFR Inhibitor CLN-081 to EGFR Exon 20 Insertion Mutations
Kagawa, Yosuke
Hayashida, Takuma
Liu, Jie
Mori, Shunta
Izumi, Hiroki
Kumagai, Shogo
Udagawa, Hibiki
Hattori, Noboru
Goto, Koichi
Kobayashi, Susumu S.
JTO CLINICAL AND RESEARCH REPORTS, 2023, 4 (03):
[5] JIN-A02, a fourth-generation, highly effective tyrosine kinase inhibitor with intracranial activity, targeting EGFR C797S mutations in NSCLC
Yun, M. R.
Yu, M. R.
Duggirala, K. B.
Lee, K.
Lim, S. M.
Jo, A.
Seah, E.
Kim, C.
Cho, B. C.
ANNALS OF ONCOLOGY, 2022, 33 (07) : S1010 - S1011
[6] Potent in vitro activity of Tarloxotinib for EGFR C797S and other mutations refractory to current EGFR tyrosine kinase inhibitors
Suda, Kenichi
Nishino, Masaya
Koga, Takamasa
Fujino, Toshio
Kobayashi, Yoshihisa
Mitsudomi, Tetsuya
Vellanki, Avanish
Tirunagaru, Vijaya G.
CANCER RESEARCH, 2019, 79 (13)
[7] Recent Advances on the Role of EGFR Tyrosine Kinase Inhibitors in the Management of NSCLC With Uncommon, Non Exon 20 Insertions, EGFR Mutations
Passaro, Antonio
Mok, Tony
Peters, Solange
Popat, Sanjay
Ahn, Myung-Ju
de Marinis, Filippo
JOURNAL OF THORACIC ONCOLOGY, 2021, 16 (05) : 764 - 773
[8] Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions
Floc'h, Nicolas
Martin, Matthew J.
Riess, Jonathan W.
Orme, Jonathan P.
Staniszewska, Anna D.
Menard, Ludovic
Cuomo, Maria Emanuela
O'Neill, Daniel J.
Ward, Richard A.
Finlay, M. Raymond V.
McKerrecher, Darren
Cheng, Mingshan
Vang, Daniel P.
Burich, Rebekah A.
Keck, James G.
Gandara, David R.
Mack, Philip C.
Cross, Darren A. E.
MOLECULAR CANCER THERAPEUTICS, 2018, 17 (05) : 885 - 896
[9] Compound A, a fourth-generation allosteric inhibitor, a potent and highly selective EGFR with L858R activating and C797S resistance mutations for the treatment of NSCLC
Byeon, Yeji
Jung, Seung Hee
Yoon, Daseul
Kang, Seock Yong
Park, Jiyeon
Jo, Hyeim
Choi, Seong-Il
Park, Somyi
Lee, Seung-chul
Tae, Yang Hun
Kim, Tae Min
Cho, Sung-Yup
Kim, Soyeon
Ko, Donghyun
Kim, Dong-Kyu
Kim, Dong-Wan
CANCER RESEARCH, 2022, 82 (12)
[10] Non-covalent EGFR T790M targeting TKIs inhibit AZD9291 resistant EGFR C797S mutants
Robichaux, Jacqulyne P.
Nilsson, Monique
Heymach, John V.
CANCER RESEARCH, 2017, 77

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