regorafenib

Regorafenib is an orally administered small molecule multi-kinase inhibitor used primarily in the treatment of metastatic colorectal cancer, unresectable or metastatic gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC) after progression on other therapies. It works by inhibiting multiple membrane-bound and intracellular kinases involved in oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. Key targets include VEGF receptors 1–3, RET, KIT, PDGFR-alpha/beta, FGFR1/2, Tie2 (angiopoietin receptor), DDR2, EphA2 (Ephrin type-A receptor 2), TrkA (tropomyosin receptor kinase A), RAF-1, BRAF/BRAFV600E mutations among others. This broad inhibition results in anti-proliferative effects on cancer cells as well as anti-angiogenic activity that disrupts blood supply to tumors. Regorafenib was developed by Bayer and received FDA approval for colorectal cancer in 2012; its indications have since expanded to GIST and HCC.

Brand names

Stivarga

Other names

regorafenibBAY 73-4506BAY73-4506BAY-73-4506Stivarga