Drug intelligence / Profile preview

regorafenib + PD-1 antibody

Development stage
Phase 2
Lead developer
Sun Yat-sen University
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

regorafenib + PD-1 antibody is an investigational combination therapy being evaluated by Sun Yat-sen University for the treatment of metastatic colorectal cancer, particularly in patients with microsatellite stable (MSS) or mismatch repair proficient (pMMR) tumors. This regimen combines regorafenib, a small-molecule multi-kinase inhibitor that targets pathways involved in angiogenesis (VEGFR1-3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF), and the tumor microenvironment (PDGFR, FGFR, CSF1R), with a PD-1 checkpoint inhibitor. The PD-1 antibody component (such as nivolumab or toripalimab) blocks the interaction between the PD-1 receptor on T cells and its ligands, thereby enhancing the immune system's ability to identify and destroy cancer cells. Clinical trials at Sun Yat-sen University have also explored the addition of radiotherapy to this combination to potentially synergize with the immunotherapy and improve objective response rates in previously treated patients.

Other names
regorafenib and PD-1 antibodyregorafenib plus PD-1 inhibitorREGONIVO
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BRAF (B-Raf proto-oncogene, serine/threonine kinase)CSF1R (Macrophage colony-stimulating factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)EPHA2 (Ephrin type-A receptor 2)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)NTRK1 (Tropomyosin-related receptor kinase A)PDCD1 (Programmed cell death protein 1 receptor)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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