Enozertinib Is a Selective, Brain-Penetrant EGFR Inhibitor for Treating Non-Small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations.

doi:10.1158/0008-5472.CAN-25-3502

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Article

Enozertinib Is a Selective, Brain-Penetrant EGFR Inhibitor for Treating Non-Small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations.

Cancer research - 2 Feb 2026

Junttila Melissa R, Repellin Claire E, Salaniwal Sumeet, Warne Robert, Lee Younho, Kim Haelee, Seo Kyung Ah, Lee Youngyi, Jung Hong-Ryul, Baik Jason, Chang Jae H, Andreatta Gina, Long Jason E, Sun Jessica D, Ni Stephanie W, Soroceanu Liliana, Sambucetti Lidia C, Das Akash, Chan Brenda, Narayanan Padmini, Pereira Ashley S, Chow Maneval Edna, Multani Pratik S, Patel Rupal, Panuwat Matt, Blank Brian R, Ndubaku Chudi, Romero F Anthony, Daemen Anneleen, Spira Alexander I, Friedman Lori S

Abstract excerpt

EGFR mutations are common oncogenic drivers in non-small cell lung cancer (NSCLC), and approximately half of patients develop brain metastases over the course of their disease. Patients with nonclassic EGFR mutations, such as insertions in exon 20, are a high unmet need with a worse prognosis compared with patients with classic EGFR mutations. Here, we describe the discovery and development of enozertinib...

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PMID: 41196054
DOI: 10.1158/0008-5472.CAN-25-3502

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