Last reviewed 2026-04-20 · How we verify

REGORAFENIB

Regorafenib inhibits multiple kinases involved in oncogenesis, angiogenesis, metastasis, and tumor immunity.

Regorafenib is a multi-kinase inhibitor marketed for the treatment of metastatic colorectal cancer, holding a significant position in this indication. Its key strength lies in its mechanism of action, which targets multiple pathways involved in oncogenesis, angiogenesis, metastasis, and tumor immunity, providing a comprehensive therapeutic approach. The primary risk is the key composition patent expiry in 2028, which could lead to increased competition from generic versions.

At a glance

Mechanism of action

Regorafenib works by blocking various kinases that play roles in cancer development, blood vessel formation, spread of cancer, and immune response to tumors. This helps to slow down or stop tumor growth and spread.

Approved indications

• Metastatic Colorectal Cancer
• Locally Advanced, Unresectable or Metastatic GIST
• Hepatocellular Carcinoma

Boxed warnings

• WARNING: HEPATOTOXICITY • Severe and sometimes fatal hepatotoxicity has occurred in clinical trials [see Warnings and Precautions ( 5.1 )] . • Monitor hepatic function prior to and during treatment [see Warnings and Precautions ( 5.1 )]. • Interrupt and then reduce or discontinue STIVARGA for hepatotoxicity as manifested by elevated liver function tests or hepatocellular necrosis, depending upon severity and persistence [see Dosage and Administration ( 2.2 )] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. • Severe and sometimes fatal hepatotoxicity has occurred in clinical trials. ( 5.1 ) • Monitor hepatic function prior to and during treatment. ( 5.1 ) • Interrupt and then reduce or discontinue STIVARGA for hepatotoxicity as manifested by elevated liver function tests or hepatocellular necrosis, depending upon severity and persistence. ( 2.2 )

Common side effects

• Asthenia/fatigue
• Pain
• Fever
• Decreased appetite and food intake
• HFSR/PPES
• Rash
• Diarrhea
• Mucositis
• Weight loss
• Infection
• Hypertension
• Hemorrhage

Drug interactions

• Strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital, and St. John's Wort)
• Strong CYP3A4 inhibitors (e.g., clarithromycin, grapefruit juice, itraconazole, ketoconazole, nefazodone, posaconazole, telithromycin, and voriconazole)
• BCRP substrates (e.g., methotrexate, fluvastatin, atorvastatin)

Key clinical trials

• Dose-escalation of Regorafenib in Advanced Hepatocellular Carcinoma (PHASE2)
• Regorafenib and Yttrium-90 Radioembolization for Unresectable Hepatocellular Carcinoma (PHASE2)
• Neoadjuvant Regorafenib in Combination With Nivolumab and Short-course Radiotherapy in Stage II-III Rectal Cancer (PHASE2)
• Regorafenib for Recurrent Meningioma (MIRAGE Trial) (PHASE2)
• Lenvatinib or Regorafenib for Advanced Hepatocellular Carcinoma After Immunotherapy (REVIVE) (PHASE2)
• Regorafenib in Patients With Refractory Primary Bone Tumors (PHASE1, PHASE2)
• A Study of Continued Treatment With Regorafenib in Participants With Solid Tumors Who Have Participated in Other Bayer Studies (PHASE2)
• TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (PHASE2)

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• REGORAFENIB CI brief — competitive landscape report
• REGORAFENIB updates RSS · CI watch RSS