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GFH375 + cetuximab
- Development stage
- Phase 3
- Lead developer
- GenFleet Therapeutics
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
GFH375 + cetuximab is an investigational combination regimen consisting of GFH375 (also known as VS-7375), an oral, small-molecule KRAS G12D (ON/OFF) inhibitor, and cetuximab, an approved anti-EGFR monoclonal antibody. GFH375 binds non-covalently to both the active (GTP-bound) and inactive (GDP-bound) states of KRAS G12D, blocking downstream signaling and tumor cell proliferation. Cetuximab is added to block EGFR-driven feedback reactivation of the MAPK pathway, which is a common resistance mechanism to KRAS inhibition. The combination is being developed by GenFleet Therapeutics (which retains rights in China) and Verastem Oncology (which licensed global rights outside of China). It is being evaluated in clinical trials for KRAS G12D-mutant advanced solid tumors, including metastatic colorectal cancer (mCRC), non-small cell lung cancer (NSCLC), and pancreatic ductal adenocarcinoma (PDAC).
- Other names
- GFH375 + cetuximabGFH375 plus cetuximabGFH-375 plus cetuximabGFH 375 plus cetuximabVS-7375 + cetuximabVS-7375 plus cetuximabVS7375 plus cetuximabVS 7375 plus cetuximab
02
Targets
EGFR (Epidermal growth factor receptor)KRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)RAF1 (c-Raf-1 (Y340D/Y341D))
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