Regorafenib is a kinase inhibitor used to treat patients with metastatic colorectal cancer, unresectable, locally advanced, or metastatic gastrointestinal stromal tumors, and hepatocellular carcinoma. Regorafenib is an orally-administered inhibitor of multiple kinases.
- Mechanism
- Curator reviewed
Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma.
- Primary indication
- Regorafenib is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy.Curator reviewed · 6 structured indications
- Formula / weight
- C21H15ClF4N4O3 · 482.815 g/mol (avg)
- First approval
- Canada, 2013 · United States, 2012 · European Union, 2016
- Code names
- BAY 73-4506
- Brand names
Resolves to
FNHKPVJBJVTLMP-UHFFFAOYSA-NSMILESCNC(=O)C1=CC(OC2=CC(F)=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)=CC=N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Regorafenib, and which of those have an active Phase 3 trial?
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