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Regorafenib (BAY73-4506)
Regorafenib is a multikinase inhibitor that blocks multiple receptor tyrosine kinases involved in tumor angiogenesis, stromal signaling, and oncogenic signaling.
Regorafenib is a multikinase inhibitor that blocks multiple receptor tyrosine kinases involved in tumor angiogenesis, stromal signaling, and oncogenic signaling. Used for Metastatic colorectal cancer (second-line or later), Gastrointestinal stromal tumor (GIST) after imatinib and sunitinib failure, Hepatocellular carcinoma.
At a glance
| Generic name | Regorafenib (BAY73-4506) |
|---|---|
| Sponsor | Bayer |
| Drug class | Multikinase inhibitor |
| Target | VEGFR1-3, FGFR, TIE2, KIT, RET, RAF-1, BRAF |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Regorafenib inhibits a broad spectrum of kinases including VEGFR1-3, FGFR, TIE2, KIT, RET, RAF-1, and BRAF. By targeting both tumor vasculature (angiogenesis) and tumor cell proliferation pathways, it disrupts multiple mechanisms that support tumor growth and progression. This multikinase approach is particularly effective in advanced colorectal and gastrointestinal stromal tumors.
Approved indications
- Metastatic colorectal cancer (second-line or later)
- Gastrointestinal stromal tumor (GIST) after imatinib and sunitinib failure
- Hepatocellular carcinoma
Common side effects
- Hand-foot skin reaction
- Diarrhea
- Fatigue
- Hypertension
- Rash
- Mucositis
- Hemorrhage
Key clinical trials
- Regorafenib and Yttrium-90 Radioembolization for Unresectable Hepatocellular Carcinoma (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)
- Phase II Study of Regorafenib as Maintenance Therapy (PHASE2)
- Regorafenib in Metastatic Colorectal Cancer : a Cohort Study in the Real-life Setting
- Phase II Study of Regorafenib in Metastatic Soft Tissue Sarcoma (PHASE2)
- Regorafenib-pembrolizumab vs. TACE/TARE in Intermediate Stage HCC Beyond Up-to-7 (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Regorafenib (BAY73-4506) CI brief — competitive landscape report
- Regorafenib (BAY73-4506) updates RSS · CI watch RSS
- Bayer portfolio CI