Drug intelligence / Profile preview

GFH375 + panitumumab

Development stage
Phase 2
Lead developer
GenFleet Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
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Overview

GFH375 + panitumumab is an investigational combination therapy being evaluated for the treatment of KRAS G12D-mutant metastatic colorectal cancer (mCRC). The regimen combines GFH375 (also known as VS-7375), an orally bioavailable, highly selective small-molecule inhibitor that targets both the active (ON) and inactive (OFF) states of the KRAS G12D mutant protein, with panitumumab, a recombinant human IgG2 monoclonal antibody directed against the epidermal growth factor receptor (EGFR). In colorectal cancer, inhibition of KRAS often triggers compensatory feedback activation of EGFR, which reactivates downstream MAPK signaling and leads to drug resistance. By concurrently blocking EGFR with panitumumab and KRAS G12D with GFH375, this combination therapy aims to achieve synergistic pathway blockade and overcome resistance mechanisms. The combination is currently undergoing clinical evaluation in Phase II trials.

Other names
GFH375 plus panitumumabGFH-375 plus panitumumabGFH 375 plus panitumumabVS-7375 + panitumumabVS-7375 plus panitumumabVS7375 plus panitumumabVS 7375 plus panitumumab
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