Drug intelligence / Profile preview

sintilimab + regorafenib

Development stage
Phase 2
Lead developer
Innovent Biologics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

Sintilimab + regorafenib is a combination therapy consisting of sintilimab, a monoclonal antibody targeting the programmed cell death protein 1 (PD-1), and regorafenib, an oral small molecule multikinase inhibitor. Sintilimab acts as an immune checkpoint inhibitor by blocking PD-1 on T cells, thereby enhancing antitumor immune responses. Regorafenib inhibits multiple kinases involved in tumor angiogenesis (such as VEGFR), oncogenesis, and the tumor microenvironment. This combination has been investigated primarily for advanced or metastatic cancers that are refractory to standard therapies, including microsatellite stable metastatic colorectal cancer (MSS mCRC) and hepatocellular carcinoma (HCC). Clinical studies have shown that this regimen can improve overall survival and response rates compared to monotherapy with either agent alone, with a manageable safety profile[1][2][3][8].

Brand names
Tyvyt (sintilimab)Stivarga (regorafenib)
Other names
rego-sintilimab
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)FGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)PDCD1 (Programmed cell death protein 1 receptor)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)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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