A halogenated-heteroaryl kinase inhibitor for treating soft tissue sarcoma and vascular tumors
The halogenated heterocyclic kinase inhibitor E9 addresses the limitations of current angiosarcoma treatments by targeting SIK3 kinase, achieving prolonged progression-free survival and enhanced treatment response through immune modulation and tumor inhibition.
Patent Information
- Application Number
- PCT/EP2025/061968
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-10-22
- Filing Date
- 2025-04-30
- Publication Date
- 2025-11-06
AI Technical Summary
Current treatments for soft tissue sarcomas, particularly angiosarcoma, are insufficient, with surgery often incomplete, radiotherapy having limited efficacy, and chemotherapy causing severe side effects and drug resistance, necessitating the development of more effective targeted therapies.
A halogenated heterocyclic kinase inhibitor, compound E9, targets SIK3 kinase to inhibit tumor growth and enhance immune response, potentially combined with other therapies like immune therapies or chemotherapeutics, providing prolonged progression-free survival and extended treatment response.
Compound E9 demonstrates significant tumor growth inhibition and improved survival outcomes in angiosarcoma models by downregulating Src-family kinases, offering a novel targeted treatment option with reduced side effects.