Quinazoline compounds for inducing degradation of G12D mutant KRAS protein
JP2026048973A5Pending Publication Date: 2026-05-25ASTELLAS PHARMA INC
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Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- ASTELLAS PHARMA INC
- Filing Date
- 2025-12-24
- Publication Date
- 2026-05-25
AI Technical Summary
Technical Problem
Current treatments for pancreatic cancer, particularly those targeting G12D mutant KRAS, are ineffective, and there is a need for highly effective therapeutic agents that can induce the degradation of this specific mutant protein.
Method used
A quinazoline compound linked with an E3 ligase ligand through a linker, forming a bifunctional compound that induces the degradation of G12D mutant KRAS protein, serving as a G12D mutant KRAS inhibitor.
Benefits of technology
The compound effectively degrades G12D mutant KRAS protein, offering a potential therapeutic agent for pancreatic cancer, especially G12D mutant KRAS-positive pancreatic cancer, including metastatic, locally advanced, recurrent, or refractory cases.
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Abstract
This invention provides compounds useful as active ingredients in pharmaceutical compositions for the treatment of pancreatic cancer. [Solution] The present inventors investigated compounds useful as active ingredients in pharmaceutical compositions for the treatment of pancreatic cancer and found that quinazoline compounds have an excellent ability to induce the degradation of G12D mutant KRAS protein and possess G12D mutant KRAS inhibitory activity, and can be used as a therapeutic agent for pancreatic cancer, thus completing the present invention. The quinazoline compound or a salt thereof of the present invention can be used as a therapeutic agent for pancreatic cancer.
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