Cardiac safety and toxicity minimization of regorafenib treatment

摘要

Regorafenib is a small molecule inhibitor of a number of protein kinases, including those involved in tumor angiogenesis (VEGFR-1, -2 and -3, TIE2), oncogenesis {KIT, RET, RAF1, BRAF, BRAFV600E) arid maintenance of the tumor microenvironment (PDGFR, FGFR) [1].Regorafenib has been approved by the US FDA and the EMA in the treatment of metastatic gastrointestinal stromal tumors (GIST) and colorectal cancer. Based on the results of the GRID Phase III clinical trial, regorafenib has established itself as the standard third-line option in the treatment of advanced GIST patients failing imatinib and sunitinib [2]. In the CORRECT Phase III trial, single-agent regorafenib also showed activity in the treatment of heavily pretreated metastatic colorectal cancer patients, with a statistically significant overall survival benefit of 1.4 months [3].