Treatment methods for subjects with non-small cell lung cancer having an aberration in EGFR

Zipalertinib, a selective EGFR tyrosine kinase inhibitor, addresses the poor treatment outcomes for NSCLC with EGFR exon 20 mutations by providing effective and tolerable antitumor activity with reduced adverse effects, particularly in patients who have received prior systemic treatments.

WO2025006697A1PCT designated stage expired Publication Date: 2025-01-02TAIHO PHARMA CO LTD
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Patent Information

Application Number
PCT/US2024/035743
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-05-22
Filing Date
2024-06-27
Publication Date
2025-01-02

AI Technical Summary

Technical Problem

Current treatments for non-small cell lung cancer (NSCLC) with EGFR exon 20 insertion mutations have poor outcomes and are associated with adverse effects, with limited effective and tolerable options, particularly in the front-line setting and for patients who have progressed after platinum-based chemotherapy.

Method used

The use of zipalertinib (CLN-081/TAS6417), a novel EGFR tyrosine kinase inhibitor with high selectivity for EGFR mutations, including exon 20 insertions, which is administered orally to patients who have previously received systemic treatments, offering a more favorable safety profile and increased efficacy compared to existing therapies.

Benefits of technology

Zipalertinib demonstrates potent antitumor activity with reduced adverse effects, achieving significant tumor regression and prolonged progression-free survival in patients with EGFR exon 20 insertion mutations, including those with metastatic disease and brain metastases, while maintaining a favorable side-effect profile.

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Abstract

A method of treating a subject with a cancer having at least one aberration in EGFR, whereby the subject is administered (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide (also known as zipalertinib and as TAS6417) or a pharmaceutically acceptable salt thereof, to a subject who has previously been treated with a molecularly targeted therapeutic. The molecularly targeted therapeutic may be an EGFR-targeting therapeutic other than Compound (1) or a non-EGFR-targeting therapeutic. The method may optionally involve administering to the subject an additional therapeutic agent.
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Citation Information

Patent Citations

  • Selective inhibitor of exon 20 insertion mutant EGFR

    US20190262345A1

  • Exon 18 and / or exon 21 mutant EGFR selective inhibitor

    US20200253975A1

  • Method to determine responsiveness of cancer to epidermal growth factor receptor targeting treatments

    US20210017604A1

  • Osimertinib for use in the treatment of non-small cell lung cancer

    US20220175783A1

  • Treatment regimens for EXON-20 insertion mutant EGFR cancers

    WO2022055895A1

Cited By

  • Methods for treatment of non-small cell lung cancers

    WO2025250276A1