Drug intelligence / Profile preview

regorafenib + anti-PD-1 antibodies

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

Overview

Regorafenib + anti-PD-1 antibodies is a combination therapy consisting of regorafenib, an oral small molecule multi-kinase inhibitor, and monoclonal antibodies targeting programmed cell death protein 1 (PD-1). Regorafenib inhibits multiple kinases involved in tumor angiogenesis (such as VEGFR), oncogenesis (including KIT, RET), and the tumor microenvironment (CSF1R, FGFR). Anti-PD-1 antibodies block the PD-1 immune checkpoint on T cells, enhancing antitumor immune responses. The combination has shown synergistic effects in preclinical models by normalizing tumor vasculature, increasing CD8+ T-cell infiltration via CXCL10/CXCR3 signaling, reducing immunosuppressive macrophages and regulatory T cells, and improving overall antitumor efficacy. Clinically investigated primarily for advanced or refractory solid tumors such as microsatellite stable metastatic colorectal cancer (MSS mCRC) and hepatocellular carcinoma (HCC), this regimen demonstrates promising efficacy with manageable safety profiles[4][5][6][8][9].

Other names
regorafenib plus anti-PD-1 antibodyregorafenib plus PD-1 inhibitorregorafenib/anti-PD1 combination therapy
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)PDGFRB (Platelet-derived growth factor receptor beta)PDCD1 (Programmed cell death protein 1 receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR (FGFR family)

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