Macrocyclic RAS inhibitor
JP2025521232A5Pending Publication Date: 2026-06-16REVOLUTION MEDICINES INC
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- REVOLUTION MEDICINES INC
- Filing Date
- 2023-06-09
- Publication Date
- 2026-06-16
AI Technical Summary
Technical Problem
Current drug discovery efforts have been largely unsuccessful in targeting the 'on' form of Ras proteins, which are implicated in approximately 30% of human cancers, due to their refractory nature to small-molecule modulation.
Method used
Development of Ras inhibitors that form a high-affinity tri-complex with the Ras protein and cyclophilin A, creating a novel binding pocket to sterically occlude the interaction site required for oncogenic signaling, thereby inhibiting Ras(ON).
Benefits of technology
The inhibitors effectively target Ras(ON), potentially providing therapeutic options for cancers driven by various Ras mutations by disrupting oncogenic signaling pathways.
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Smart Images
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Abstract
The present disclosure features macrocyclic compounds capable of inhibiting Ras proteins, as well as pharmaceutical compositions and protein complexes thereof, and their use in cancer treatment.
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