Management of regorafenib-related toxicities: a review

• Main Authors: Saravanan K. Krishnamoorthy, Valerie Relias, Sunit Sebastian, Vijay Jayaraman, Muhammad Wasif Saif
• Format: Article
• Language: English
• Published: SAGE Publishing 2015-09-01
• Series: Therapeutic Advances in Gastroenterology
• Online Access: https://doi.org/10.1177/1756283X15580743
• ISSN: 1756-283X; 1756-2848

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.