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Drug intelligence / Profile preview
regorafenib
- Development stage
- Approved
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Regorafenib is an orally administered small molecule multi-kinase inhibitor used primarily in the treatment of metastatic colorectal cancer, unresectable or metastatic gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC) after progression on other therapies. It works by inhibiting multiple membrane-bound and intracellular kinases involved in oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. Key targets include VEGF receptors 1–3, RET, KIT, PDGFR-alpha/beta, FGFR1/2, Tie2 (angiopoietin receptor), DDR2, EphA2 (Ephrin type-A receptor 2), TrkA (tropomyosin receptor kinase A), RAF-1, BRAF/BRAFV600E mutations among others. This broad inhibition results in anti-proliferative effects on cancer cells as well as anti-angiogenic activity that disrupts blood supply to tumors. Regorafenib was developed by Bayer and received FDA approval for colorectal cancer in 2012; its indications have since expanded to GIST and HCC.
- Brand names
- Stivarga
- Other names
- regorafenibBAY 73-4506BAY73-4506BAY-73-4506Stivarga
02
Targets
ABL2 (ABL proto-oncogene 2, 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)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)NTRK1 (Tropomyosin-related receptor kinase A)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)EPHA (EPHA receptor family)PDGFRA (Platelet-derived growth factor receptor alpha)
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