Drug glossary Targeted therapy

Regorafenib Stivarga

A drug approved for colorectal cancer. It appears in 109 clinical trials.

Oral VEGFR1 VEGFR2 VEGFR3 TIE2 PDGFR FGFR KIT RET RAF
See its trials
United States FDA approved Since 2012
European Union EMA approved Since 2013
Spain Funded by SNS Approved for colorectal cancer

What it is

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.

How it works

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

Common side effects

Hand-foot skin reactionFatigueDiarrheaDecreased appetiteHypertensionMucositisDysphoniaInfectionsLiver enzyme elevation

Not all are listed, and everyone experiences them differently. If you notice any, tell your care team.