Abstract: Targeted therapies by means of compounds that inhibit a specific target molecule represent a new perspective in the treatment of cancer. Various signaling pathways have been implicated in the development and progression of cancer. There is a general agreement that molecules interfering simultaneously with multiple targets might be more effective than single target agents. Regorafenib （BAY 73-4506） is a novel， oral multikinase inhibitor， which demonstrates a broad spectrum of antitumor activity， probably due to the targeting of several angiogenic， oncogenic and stromal kinases. On September 2012， regorafenib was approved by US Food and Drug Administration（FDA） for previously heavy treated metastatic colorectal cancer. On February 2013， US FDA expanded the approved use to treat patients with advanced gastrointestinal stromal tumors. Two large， randomized，international multicentre，phase Ⅲ clinical trial in patients with metastatic colorectal cancer and gastrointestinal stromal tumour treated by regorafenib were finished. The CORRECT trial evaluated regorafenib for the treatment of patients with metastatic colorectal cancer who had progressed after standard therapies. The results confirmed that regorafenib was associated with significant improvements in overall survival. The GRID trial showed that regorafenib could provide a significant improvement in progressionfree survival compared with placebo in patients with metastatic gastrointestinal stromal tumour following failure of imatinib and sunitinib. The toxicity profile of regorafenib is comparable with other oral multikinase inhibitors with similar molecular targets. Most toxicities associated with regorafenib are mild／moderate and clinically managable. Further extensive clinical development as a single agent or in combination with standard chemotherapeutic agents in various malignant tumors is ongoing.