Combination therapy of cancer using statinib and KRAS g12c inhibitors

The combination therapy of zogerinib and a KRAS G12C inhibitor synergistically inhibits HER2 and KRAS G12C, addressing the inadequacy of existing therapies and achieving effective treatment and tumor shrinkage for HER2-dependent and KRAS G12C-mutant cancers.

CN122458993APending Publication Date: 2026-07-24BOEHRINGER INGELHEIM INT GMBH
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Patent Information

Application Number
CN202480081404.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2024-07-12
Filing Date
2024-12-18
Publication Date
2026-07-24

AI Technical Summary

Technical Problem

Existing treatments have limited efficacy against HER2-dependent cancers and KRAS G12C-mutant cancers, and targeted therapies for KRAS mutants have resistance issues, necessitating more effective combination therapy regimens.

Method used

Zongetinib, when used in combination with KRAS G12C inhibitors (such as sotoraraxib or adagraxib), inhibits HER2 tyrosine kinase and KRAS G12C through combination therapy, achieving synergistic anti-proliferative activity and enhancing the efficacy of KRAS inhibitors.

Benefits of technology

It demonstrated synergistic effects in cancer treatment, achieving tumor shrinkage and tolerability, expanding the patient population that benefits from KRAS G12C inhibitors, and had no significant toxicity.

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Abstract

The present invention relates to a combination of a HER2 tyrosine kinase zongertinib (zongertinib) and a KRAS G12C inhibitor. The present invention also relates to a method for preparing the same. The combinations of the invention are useful in the treatment and / or prevention of oncogenic and / or hyperproliferative diseases, such as cancer. Thus, provided herein are compounds used in relation to the combination, methods of prevention and / or treatment, uses, pharmaceutical compositions, and kits.
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