As a multikinase inhibitor of of angiogenic, stromal and oncogenic receptor tyrosine kinases, Regorafenib (BAY 73-4506) can inhibit c-KIT, VEGFR-2, B-Raf with IC50 of 17 nM, 40 nM and 69 nM. Regorafenib (BAY 73-4506) also inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-beta and fibroblast growth fa1)Regorafenib showed an acceptable safety profile and preliminary evidence of antitumor activity in patients with solid tumors. (2)Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts.A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qdx5 dosing at 10 and 30 mg/kg. Regorafenib exhibited potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages observed in breast MDA-MB-231 and renal 786-O carcinoma models. (3) Regorafenib showed tolerability and antitumour activity in patients with metastatic CRC. (4) Regorafenib has significant activity in patients with advanced GIST (Metastatic GI stromal tumor) after failure of both imatinib and sunitinib.ctor receptor 1) and the mutant RET.