The European Society for Medical Oncology (ESMO) Congress was held in Copenhagen, Denmark from 7th–11th October 2016. The use of the promiscuous multikinase inhibitor regorafenib (Stivarga®, BAY 73-4506) in the treatment of cancers of the gastrointestinal (GI) tract was strongly featured at this meeting. Regorafenib targets multiple kinases involved in oncogenesis and angiogenesis, and is US Food and Drug Administration (FDA)-approved for the treatment of advanced metastatic colorectal cancer and GI stromal tumours, following progression on standard therapies. In this review, we summarise the results of completed clinical trials on the use of regorafenib alone or in combination with other therapies for the treatment of GI cancers. We highlight the results of the Phase III RESORCE study which demonstrated the efficacy of regorafenib as a second-line therapy in patients with advanced hepatocellular carcinoma who have progressed on sorafenib. We review some promising preliminary data on the use of regorafenib in other GI cancers, such as gastric cancer, oesophageal cancer, pancreatic cancer, and soft tissue carcinomas, and provide a brief overview of ongoing and planned trials. Finally, we discuss the incidence and management of regorafenib-related toxicities and summarise attempts to identify predictive biomarkers of regorafenib sensitivity.
Please view the full content in the pdf above.