Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.

doi:10.1021/acs.jmedchem.2c00893

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Article

Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.

Journal of medicinal chemistry - 13 Oct 2022

Obst-Sander Ulrike, Ricci Antonio, Kuhn Bernd, Friess Thomas, Koldewey Philipp, Kuglstatter Andreas, Hewings David, Goergler Annick, Steiner Sandra, Rueher Daniel, Imhoff Marie-Paule, Raschetti Noemi, Marty Hans-Peter, Dietzig Aline, Rynn Caroline, Ehler Andreas, Burger Dominique, Kornacker Martin, Schaffland Jeannine Petrig, Herting Frank, Pao William, Bischoff James R, Martoglio Bruno, Alice Nagel Yvonne, Jaeschke Georg

Abstract excerpt

Addressing resistance to third-generation EGFR TKIs such as osimertinib via the EGFRC797S mutation remains a highly unmet need in EGFR-driven non-small-cell lung cancer (NSCLC). Herein, we present the discovery of the allosteric EGFR inhibitor 57, a novel fourth-generation inhibitor to overcome EGFRC797S-mediated resistance in patients harboring the activating EGFRL858R mutation. 57 exhibits an improved potency...

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PMID: 36178776
DOI: 10.1021/acs.jmedchem.2c00893

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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