STIVARGA
Stivarga (regorafenib) is a kinase inhibitor indicated for the treatment of adult patients with specific advanced-stage solid tumors. It is used for metastatic colorectal cancer in patients previously treated with standard chemotherapy and targeted anti-VEGF or anti-EGFR therapies. The drug is also approved for patients with locally advanced or metastatic gastrointestinal stromal tumors (GIST) and hepatocellular carcinoma (HCC) who have received prior specific systemic treatments. Stivarga serves as a therapeutic option for patients whose disease has progressed following these earlier lines of therapy.
How STIVARGA Works
Regorafenib is a small molecule inhibitor that targets multiple membrane-bound and intracellular kinases involved in both normal and pathological cellular functions. The drug and its active metabolites block various receptors and signaling proteins, including VEGFR, KIT, and PDGFR, which are critical for tumor growth and the formation of new blood vessels. By inhibiting these targets, the medication disrupts oncogenesis, tumor angiogenesis, and metastasis. This multi-kinase inhibition also affects tumor immunity and helps suppress the spread of cancer cells within the body.
Details
- Status
- Prescription
- First Approved
- 2012-09-27
- Routes
- ORAL
- Dosage Forms
- TABLET
STIVARGA Approval History
What STIVARGA Treats
3 indicationsSTIVARGA is approved for 3 conditions since its original approval in 2012. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Metastatic colorectal cancer
- Locally advanced, unresectable or metastatic gastrointestinal stromal tumor
- Hepatocellular carcinoma
STIVARGA Boxed 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 prescribin...
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 )
STIVARGA Target & Pathway
ProTarget
A kinase in the MAPK signaling pathway that regulates cell growth. BRAF mutations (especially V600E) occur in melanoma, colorectal, and thyroid cancers, causing uncontrolled cell proliferation. Inhibiting mutant BRAF blocks this aberrant growth signal.
STIVARGA Competitors
Pro6 other drugs also target FGFR1. Compare mechanisms, indications, and trial activity.
Competitors share the same molecular target (FGFR1). Earlier expiry dates signal biosimilar/generic opportunities.
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Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
STIVARGA FDA Label Details
ProIndications & Usage
FDA Label (PDF)STIVARGA is a kinase inhibitor indicated for the treatment of adult patients with: • Metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type, an anti-EGFR therapy. • Locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. • Hepatocellular carcinoma (HCC) who have been previously treated with sorafenib 1.1 Colorectal Cancer STIVARGA is indicated for the treatment of...
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 hepato...
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Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.