Drug intelligence / Profile preview

erfonrilimab + regorafenib

Development stage
Phase 2
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.

Other names
KN046 + regorafeniberfonrilimab plus regorafenib
02

Targets

BRAF V600ECTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)FGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CD274 (Programmed cell death protein 1 ligand 1)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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