Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

Yong Jia, Cai-Hong Yun, Eunyoung Park, Dalia Ercan, Mari Manuia, Jose Juarez, Chunxiao Xu, Kevin Rhee, Ting Chen, Haikuo Zhang, Sangeetha Palakurthi, Jaebong Jang, Gerald Lelais, Michael DiDonato, Badry Bursulaya, Pierre-Yves Michellys, Robert Epple, Thomas H. Marsilje, Matthew McNeill, Wenshuo Lu, Jennifer Harris, Steven Bender, Kwok-Kin Wong, Pasi A. Jänne and Michael J. Eck ()
Additional contact information
Yong Jia: Genomics Institute of the Novartis Research Foundation
Cai-Hong Yun: Dana-Farber Cancer Institute
Eunyoung Park: Dana-Farber Cancer Institute
Dalia Ercan: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Mari Manuia: Genomics Institute of the Novartis Research Foundation
Jose Juarez: Genomics Institute of the Novartis Research Foundation
Chunxiao Xu: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Kevin Rhee: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Ting Chen: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Haikuo Zhang: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Sangeetha Palakurthi: Belfer Center for Applied Cancer Science, Dana-Farber Cancer Institute
Jaebong Jang: Dana-Farber Cancer Institute
Gerald Lelais: Genomics Institute of the Novartis Research Foundation
Michael DiDonato: Genomics Institute of the Novartis Research Foundation
Badry Bursulaya: Genomics Institute of the Novartis Research Foundation
Pierre-Yves Michellys: Genomics Institute of the Novartis Research Foundation
Robert Epple: Genomics Institute of the Novartis Research Foundation
Thomas H. Marsilje: Genomics Institute of the Novartis Research Foundation
Matthew McNeill: Genomics Institute of the Novartis Research Foundation
Wenshuo Lu: Genomics Institute of the Novartis Research Foundation
Jennifer Harris: Genomics Institute of the Novartis Research Foundation
Steven Bender: Genomics Institute of the Novartis Research Foundation
Kwok-Kin Wong: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Pasi A. Jänne: Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute
Michael J. Eck: Dana-Farber Cancer Institute

Nature, 2016, vol. 534, issue 7605, 129-132

Abstract: An allosteric inhibitor, EAI045, is reported that is selective for certain drug-resistant EGFR mutants, but spares the wild-type receptor; combination therapy of EAI045 with EGFR-dimerization-blocking antibodies is effective in mouse models of lung cancer driven by mutant versions of EGFR that are resistant to all previously developed inhibitors.

Date: 2016
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DOI: 10.1038/nature17960

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