RAS inhibitors and pharmaceutical preparations containing this compound.
Patent Information
- Application Number
- VN1202602365
- Authority / Receiving Office
- VN · VN
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2020-06-24
- Filing Date
- 2020-11-04
- Publication Date
- 2026-07-15
AI Technical Summary
Current drug discovery efforts have been largely unsuccessful in targeting 'undruggable' proteins, such as Ras proteins, which are crucial in human cancers, due to their refractory nature to small molecule modulation, with only about 10% of human proteins being targetable by small molecules, leaving a significant reservoir of medically important proteins untapped.
The formation of a high-affinity three-component complex between a synthetic ligand and the Ras protein and a cytosolic chaperone like cyclophilin A, creating a new binding pocket that sterically occludes interaction sites with downstream effector molecules, thereby inhibiting oncogenic signaling.
This approach effectively inhibits Ras protein activity by forming a high-affinity tri-complex, potentially leading to tumor regression in cancer models, as demonstrated by Compound A in pancreatic CDX models, with all dose levels well tolerated and significant tumor regression achieved.