Last reviewed 2026-05-14 · How we verify

Stivarga (regorafenib)

Stivarga blocks the activity of enzymes involved in tumor growth and angiogenesis.

Stivarga (regorafenib) is a small molecule kinase inhibitor developed by Bayer Healthcare, targeting bifunctional epoxide hydrolase 2. It is FDA-approved for treating gastrointestinal stromal tumor, liver cell carcinoma, and metastasis from malignant tumor of the colon. Stivarga is a patented medication with a half-life of 51 hours, and its commercial status is subject to change. Key safety considerations include its potential for severe side effects, such as hypertension and bleeding. As a kinase inhibitor, Stivarga works by blocking the activity of specific enzymes involved in tumor growth and angiogenesis.

At a glance

Mechanism of action

Regorafenib is small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity. 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, BRAF V600E, SAPK2, PTK5, Abl and CSF1R at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in rat tumor model and inhibition of tumor growth in several mouse xenograft models including some for human colorectal carcinoma, gastrointestinal stromal and hepatocellular carcinoma. Regorafenib also demonstrated anti-metastatic activity in mouse xenograft model and two mouse orthotopic models of human colorectal carcin

Approved indications

• Gastrointestinal stromal tumor
• Liver cell carcinoma
• Metastasis from malignant tumor of colon

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

• Pain
• HFSR
• Asthenia/Fatigue
• Diarrhea
• Decreased Appetite/Food Intake
• Hypertension
• Infection
• Dysphonia
• Hyperbilirubinemia
• Fever
• Mucositis
• Weight Loss

Drug interactions

• P-glycoprotein Substrates

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)

Patents

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:

• Stivarga CI brief — competitive landscape report
• Stivarga updates RSS · CI watch RSS
• Bayer portfolio CI