Drug intelligence / Profile preview

regorafenib + immune checkpoint inhibitor

Development stage
Unknown
Lead developer
Bayer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Regorafenib + immune checkpoint inhibitor is a combination therapy consisting of regorafenib, an oral multi-kinase inhibitor, and an immune checkpoint inhibitor (ICI), typically targeting PD-1 or PD-L1. Regorafenib inhibits multiple protein kinases involved in tumor angiogenesis (such as VEGFR), oncogenesis (such as KIT, RET), and the tumor microenvironment. Immune checkpoint inhibitors block inhibitory pathways in T cells—most commonly the PD-1/PD-L1 axis—thereby enhancing anti-tumor immunity. This combination aims to overcome resistance to immunotherapy seen in certain cancers by modulating both the tumor vasculature/microenvironment and reactivating anti-tumor immune responses. The regimen has been studied primarily in metastatic colorectal cancer, hepatocellular carcinoma, and biliary tract cancer[1][2][3][4].

02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)NTRK1 (Tropomyosin-related receptor kinase A)RAF1 (c-Raf-1 (Y340D/Y341D))CSF1R (Macrophage colony-stimulating factor receptor)EPHA2 (Ephrin type-A receptor 2)TEK (Tie2)PDGFRB (Platelet-derived growth factor receptor beta)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)

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