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erfonrilimab + regorafenib
- Development stage
- Unknown
- Lead developer
- AlphaMab Oncology
- Modality
- Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Erfonrilimab + regorafenib is a combination therapy being investigated for the treatment of metastatic microsatellite-stable (MSS) colorectal cancer. Erfonrilimab (KN046) is a novel bispecific monoclonal antibody developed by Alphamab Oncology that simultaneously targets two key immune checkpoints: programmed death-ligand 1 (PD-L1) and cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4). By blocking these pathways, erfonrilimab aims to restore and enhance the anti-tumor activity of T-cells. Regorafenib is an oral multi-kinase inhibitor that targets several pathways involved in tumor angiogenesis (VEGFR1-3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF), and the tumor microenvironment (PDGFR, FGFR). The combination is currently being evaluated in a Phase II multi-cohort study led by Peking University Cancer Hospital & Institute, specifically focusing on MSS colorectal cancer patients who often show poor responses to standard immunotherapy. The trial stratifies patients based on liver metastasis status, BRAF V600E mutation, or chemotherapy intolerance.
- Brand names
- Stivarga
- Other names
- KN046 + regorafeniberfonrilimab plus regorafenib
02
Targets
KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))PDGFRB (Platelet-derived growth factor receptor beta)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)BRAF V600EVEGFR-1 (Vascular endothelial growth factor receptor 1)CD274 (Programmed cell death protein 1 ligand 1)VEGFR3 (Vascular endothelial growth factor receptor 3)TEK (Tie2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)
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