Elironrasib — Investigational Agent
KRAS Inhibitor · Phase 1/2 · Revolution Medicines, Inc.
Mechanism of Action
Elironrasib is an oral, covalent RAS(ON) G12C-selective tri-complex inhibitor. Unlike RAS(OFF) inhibitors (sotorasib, adagrasib) that bind the inactive GDP-bound state, elironrasib forms a tri-complex with the intracellular chaperone cyclophilin A, and this complex covalently engages the active GTP-bound (ON) state of KRAS G12C, sterically blocking effector binding and downstream MAPK signaling. Targeting the active state is designed to achieve deeper pathway suppression and activity against tumors resistant to RAS(OFF) G12C inhibitors.
Investigational Indications
- KRAS G12C-mutant non-small cell lung cancer (NSCLC)
- KRAS G12C-mutant colorectal cancer (CRC)
- Other KRAS G12C-mutant advanced solid tumors, including after prior G12C inhibitor