Drug intelligence / Profile preview

regorafenib + sorafenib

Development stage
Unknown
Lead developer
Bayer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Regorafenib + sorafenib is a combination of two oral small molecule multikinase inhibitors used in the treatment of advanced cancers. Both drugs inhibit multiple protein kinases involved in tumor angiogenesis and oncogenesis. Regorafenib is approved for metastatic colorectal cancer, unresectable or metastatic gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC) after prior therapy with sorafenib[1][2]. Sorafenib is approved for advanced renal cell carcinoma and HCC. The combination itself does not have a unique approval or established clinical use as a fixed regimen; rather, regorafenib is often used sequentially after progression on sorafenib in HCC[2][3]. Both agents act by inhibiting kinases such as VEGFRs and PDGFRs to block tumor growth and angiogenesis.

Brand names
Stivarga (regorafenib)Nexavar (sorafenib)
Other names
regorafenib + sorafenib
02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)BRAF V600EVEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))

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