Ras inhibitors

WO2026090116A3PCT designated stage Publication Date: 2026-06-04REVOLUTION MEDICINES INC
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
REVOLUTION MEDICINES INC
Filing Date
2025-10-21
Publication Date
2026-06-04

AI Technical Summary

Technical Problem

Current drug discovery efforts have been largely unsuccessful in targeting the undruggable Ras proteins, which are implicated in approximately 30% of human cancers, with only two agents approved for the K-Ras G12C mutant, highlighting the need for new molecular modalities to modulate Ras protein function.

Method used

Formation of a high-affinity three-component complex between Ras proteins and the cytosolic chaperone cyclophilin A, creating a new binding pocket that sterically occludes interactions with downstream effector molecules, thereby inhibiting oncogenic signaling.

Benefits of technology

This approach provides a novel mechanism to inhibit Ras proteins, potentially offering therapeutic benefits for cancers driven by various Ras mutations, including those resistant to existing treatments.

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Abstract

The disclosure features macrocyclic compounds and pharmaceutical compositions thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
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Citation Information

Patent Citations

  • US20210130369A1

  • WO2022060583A1

  • WO2023208005A1

  • WO2024081363A1

  • WO2024149819A1