Regorafenib: A Guide to Its Use in Advanced Gastrointestinal Stromal Tumor (GIST) After Failure of Imatinib and Sunitinib

Regorafenib (Stivarga (R)), a new inhibitor of multiple kinases, is indicated as third-line treatment in patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib and sunitinib in the USA. In a phase III trial in patients with progressive GIST after failure of standard therapies, regorafenib plus best supportive care increased median progression-free survival by > 5-fold relative to best supportive care alone. Although regorafenib is associated with several specific drug-related adverse events, it is reasonably well tolerated if recommendations for dose modifications (i.e. treatment interruption, dose reductions and/or permanent treatment discontinuation based on tolerability) and other precautions are followed.