GFH375 — Investigational Agent

KRAS Inhibitor · Phase 1/2 · GenFleet Therapeutics (partnered with Verastem)

Mechanism of Action

Orally bioavailable small-molecule inhibitor that targets the KRAS G12D mutant protein in both its active (GTP-bound/ON) and inactive (GDP-bound/OFF) states, blocking effector engagement and shutting down downstream RAS-MAPK signaling in G12D-driven tumors.

Investigational Indications

• KRAS G12D-mutant NSCLC
• KRAS G12D-mutant pancreatic cancer
• KRAS G12D-mutant colorectal cancer
• Other KRAS G12D solid tumors

Key Trials