Regorafenib
Regorafenib is a targeted therapy medication known as a multi-kinase inhibitor, meaning it works by blocking multiple proteins involved in cancer growth and spread. It is prescribed to treat certain cancers including metastatic colorectal cancer, gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (liver cancer).
Regorafenib is a multi-kinase inhibitor used to treat certain metastatic cancers by blocking proteins involved in tumor growth, blood vessel formation, and cancer spread.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- L01EX05
- RxNorm
- 1312397
- Generic
- Regorafenib
- Class
- atc-l01
- Brands
- Stivarga
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Regorafenib is used to treat adults with metastatic colorectal cancer (CRC) that has progressed after standard therapies, unresectable or metastatic gastrointestinal stromal tumors (GIST) that have progressed on prior treatment with imatinib and sunitinib, and hepatocellular carcinoma (HCC) in patients who have been previously treated with sorafenib.
Regorafenib works as a small molecule inhibitor that blocks multiple membrane-bound and intracellular kinases involved in normal cellular functions and pathologic processes including oncogenesis, tumor angiogenesis, metastasis, and tumor immunity. By inhibiting these kinases, it disrupts cancer cell growth, blood supply to tumors, and spread of cancer cells.
Common side effects include hand-foot skin reaction (palmar-plantar erythrodysesthesia), fatigue, diarrhea, hypertension, and liver enzyme elevation. Liver function should be monitored regularly during treatment. Regorafenib is metabolized by CYP3A4 enzymes, so drug interactions are possible. It should not be used during pregnancy due to potential harm to the fetus.
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy