Regorafenib (
Stivarga,
BAY 73-4506; Bayer Pharma AG, Berlin, Germany) is an oral multikinase inhibitor that targets the angiogenic tumor microenvironment and oncogenic
kinases including
vascular endothelial growth factor receptor 2 (VEGFR2), VEGFR1, VEGFR3,
fibroblast growth factor receptor 1 (FGFR1), RAF, KIT, RET and BRAF. Its antiangiogenic effect is greater than that of its related
drug,
sorafenib.
Regorafenib has been approved by the US Food and Drug Administration (FDA) for the treatment of metastatic
colorectal cancer (mCRC) in patients who have failed treatment with fluoropyrimidine,
oxaliplatin and
irinotecan based
chemotherapy, an anti-
VEGF therapy and, if KRAS wild type, an anti-EGFR
therapy. The FDA based this approval on data from the CORRECT trial, which showed the efficacy of
regorafenib compared with placebo. The most common grade 3-4 adverse reactions with the
drug are hand foot skin reactions (HFSR),
diarrhea,
hypertension and
fatigue. This review discusses the efficacy data, and the incidence and management of
regorafenib's toxicities.