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Therap Adv Gastroenterol. 2015 Sep;8(5):285-97. doi: 10.1177/1756283X15580743.

Management of regorafenib-related toxicities: a review.

Author information

1
Columbia University Medical Center, New York, New York, USA.
2
Division of Hematology/Oncology and Experimental Therapeutics, Tufts Medical Center, Boston, MA, USA.
3
University of Mississippi, Jackson, MS, USA.
4
University of Connecticut, Farmington, CT, USA.
5
Department of Medicine and Cancer Center, Tufts Medical Center, 800 Washington Street Box 245, Boston, MA 02111, USA.

Abstract

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.

KEYWORDS:

colon cancer; hypertension; metastatic; rash; regorafenib

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