Joint use of FAK inhibitor and KRAS g12c inhibitor

Through the combined use of FAK inhibitors and KRAS G12C inhibitors, the problems of limited efficacy and drug resistance of KRAS G12C inhibitors were solved, and the enhanced therapeutic effect on KRAS mutant cancer was achieved.

WO2025157162A1 Publication Date: 2025-07-31INXMED (NANJING) CO LTD
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Patent Information

Application Number
PCT/CN2025/073859
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-03-13
Filing Date
2025-01-22
Publication Date
2025-07-31

AI Technical Summary

Technical Problem

The existing KRAS G12C inhibitors have limited efficacy in the treatment of KRAS mutant cancers, and after resistance to KRAS G12C inhibitors, they target apoptotic responses through feedback-resistant FAK-YAP signaling pathway.

Method used

The FAK inhibitor is combined with KRAS G12C inhibitors, including the combination of Defactinib, AMP945, APG-2449, Conteltinib and its deuterated compounds with RMC-4998, Divarasib, LY3537982, Opnurasib, etc., to enhance the anti-tumor effect.

Benefits of technology

The therapeutic effect on KRAS mutant cancers has been enhanced, especially in cancer patients with KRAS G12C mutations, which significantly improves the synergistic effect of anti-tumor response.

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Abstract

The present invention relates to the use of a FAK inhibitor in preparing a drug to be jointly used with a KRAS G12C inhibitor to treat a tumor.
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