Regorafenib (Stivarga)
Targeted Therapy · Approved since 2012
Description
Regorafenib is an oral multi-kinase inhibitor approved for treatment of metastatic colorectal cancer in patients who have progressed after standard therapies including fluoropyrimidine, oxaliplatin, irinotecan, anti-VEGF therapy, and anti-EGFR therapy (if RAS wild-type). It serves as a third-line or later treatment option for refractory metastatic disease. The drug demonstrates activity across different molecular subtypes of CRC, including both microsatellite stable (MSS) and microsatellite instability-high (MSI-H) tumors.
Mechanism of Action
Regorafenib inhibits multiple protein kinases involved in oncogenesis, angiogenesis, and maintenance of the tumor microenvironment, including VEGFR1-3, TIE2, PDGFR, FGFR, KIT, RET, and RAF kinases. By blocking these pathways simultaneously, it disrupts tumor cell proliferation, tumor angiogenesis, and metastasis. The multi-targeted approach helps overcome resistance mechanisms that develop against single-pathway inhibitors.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Stivarga |
| Category | Targeted Therapy |
 Status | FDA Approved |
 EMA Status | EMA Approved |
 Spain Access | Funded by SNS approved in CRC |
| Administration | Oral |
| Year Approved | 2012 |
| Clinical Trials | 109 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.