Compound

Regorafenib

Also called Stivarga, A1JCR

Original Wikipedia articleen.wikipedia.org/wiki/Regorafenib revision used (24 October 2026)

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Part of the metabolic pathway of Regorafenib. See the timeline on the metabolic highway.

Enzymes that break it down: UGT1A9. Wikipedia’s drug infobox says: “Liver (UGT1A9-mediated)” (revision 1355063551).

Overview

Regorafenib, sold under the brand name Stivarga among others, is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. Since 2009 it was studied as a potential treatment option in multiple tumor types. By 2015 it had two US approvals for advanced cancers.[1] WP

Risks and side effects

Adverse effects

Regorafenib is being approved with a Boxed Warning alerting patients and health care professionals that severe and fatal liver toxicity occurred in patients treated with regorafenib during clinical studies. Serious side effects, which occurred in less than one percent of patients, were liver damage, severe bleeding, blistering and peeling of skin, very high blood pressures requiring emergency treatment, heart attacks and perforations (holes) in the intestines. The most common side effects reported in patients treated with regorafenib include weakness or fatigue, loss of appetite, hand-foot syndrome (also called palmar-plantar erythrodysesthesia), diarrhea, mouth sores (mucositis), weight loss, infection, high blood pressure, and changes in voice volume or quality (dysphonia).[2] WP

Chemistry

Formula: C21H15ClF4N4O3 PC
CAS number: 755037-03-7 PC
Molar mass (g/mol): 482.8 PC
IUPAC name (computed by PubChem): 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide PC
SMILES: CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F PC
InChIKey: FNHKPVJBJVTLMP-UHFFFAOYSA-N PC
PubChem CID: 11167602

Harm reduction information

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Sources

Other Bayer Announces New Data on Oncology Portfolio To Be Presented at the ECCO-ESMO Congress 2009
Journal / agency FDA Prescribing Information. September 27, 2012

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.