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Article

CZC54252 overcomes Osimertinib resistance by targeting EGFRC797S mutations.

BMC pharmacology & toxicology - 22 Apr 2026

Ma Tingnan, Yuan Tao, Hou Yingying, Liu Maoyu, Zhang Yaru, Shi Jianyou, Zhong Lei

Abstract excerpt

BACKGROUND: The introduction of EGFR inhibitors has revolutionized the management of NSCLC, leading to a significant extension of survival in the target patient population. Unfortunately, acquired resistance appears to be unavoidable, which restricts the use of EGFR-TKIs in the clinic. EGFRC797S represents a novel resistant mutation after treatment with the latest generation of EGFR inhibitor Osimertinib....

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Identifiers

PMID: 42021316
DOI: 10.1186/s40360-026-01139-7
PMCID: PMC13244908

Genes

EGFR
PC

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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CZC54252 overcomes Osimertinib resistance by targeting EGFRC797S mutations.PMID 42021316Read ↗

Repurposing CZC54252 to target EGFR C797S mutations and conquer Osimertinib resistanceSemantic proximity Read ↗

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Structure-guided discovery of a potent 2-aryl-4-aminoquinazoline-based inhibitor overcoming osimertinib resistance driven by EGFR C797S mutation in NSCLC.Semantic proximity Read ↗

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Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Semantic proximity Read ↗

LS-106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo.Semantic proximity Read ↗

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