Class/mechanism: Small molecule inhibitor of multiple tyrosine kinases, such as: VEGFR1, VEGFR2, VEGFR3, KIT, RET, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, Trk2A, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl, which are involved in tumor cell proliferation, survival, and angiogenesis. Its major active metabolites are M-2 and M-5.
Black Box Warning: Severe and sometimes fatal hepatotoxicity has been observed in clinical trials. Monitor hepatic function prior to and during treatment. Interrupt and then reduce or discontinue regorafenib for hepatotoxicity as manifested by elevated liver function tests (LFTs) or hepatocellular necrosis, depending upon severity and persistence.
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.
Diseases for which it is used
- Colon cancer
- Gastric cancer
- Gastrointestinal stromal tumor
- Hepatocellular carcinoma
- Renal cell carcinoma
- Soft tissue sarcoma
Patient drug information
- Regorafenib (Stivarga) package insert
- Regorafenib (Stivarga) patient drug information (Chemocare)
- Regorafenib (Stivarga) patient drug information (UpToDate)
History of changes in FDA indication
- 9/27/2012: Approved for patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy.
- 2/25/2013: Approved for patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to other FDA-approved treatments for this disease.
- 4/27/2017: Approved for the treatment of patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.
Also known as
- Code name: BAY 73-4506
- Brand names: Nublexa, Regonix, Renib, Resihance, Stivarga