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[摘要]:Regorafenib is an orally active inhibitor of VEGFR-2 and -3, c-Kit, TIE-2, PDGF-R-beta, FGFR-7, Ret, c-RAF and MAP kinase p38. Preclinical in vitro and in vivo studies demonstrate a broad spectrum of activity, likely due to the targeting of several angiogenic, stromal and oncogenic kinases. In early phase I and II studies, regorafenib has been shown to be well tolerated and demonstrated notable antitumor activity Regorafenib is currently undergoing extensive clinical development in patients with advanced renal cell cancer, colorectal cancer, non-small cell lung cancer, hepatocellular carcinoma and gastrointestinal stromal tumors. |
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