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SYHA1813 + regorafenib
- Development stage
- Unknown
- Lead developer
- Shanghai Runshi Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**SYHA1813 + regorafenib** is a combination of two orally available small molecule multi-kinase inhibitors targeting various receptor tyrosine kinases involved in tumor angiogenesis, stromal regulation, and oncogenic signaling. SYHA1813 selectively inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3) and colony-stimulating factor 1 receptor (CSF1R), impairing angiogenesis and macrophage-mediated tumor microenvironment signaling. It activates the p53 pathway and impairs DNA repair in tumor cells[1][3][5]. Regorafenib inhibits multiple kinases including RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, and TrkA, disrupting angiogenic, stromal, and oncogenic signaling pathways[2][6][8].
- Other names
- REGORAFENIBRégorafénibRegorafenibum
02
Targets
RAF1 (c-Raf-1 (Y340D/Y341D))BRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)NTRK1 (Tropomyosin-related receptor kinase A)PDGFRB (Platelet-derived growth factor receptor beta)TEK (Tie2)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)
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