瑞戈非尼相关毒性的管理：综述
Management of regorafenib-related toxicities: a review.
作者信息
Krishnamoorthy Saravanan K, Relias Valerie, Sebastian Sunit, Jayaraman Vijay, Saif Muhammad Wasif
机构信息
Columbia University Medical Center, New York, New York, USA.
Division of Hematology/Oncology and Experimental Therapeutics, Tufts Medical Center, Boston, MA, USA.
出版信息
Therap Adv Gastroenterol. 2015 Sep;8(5):285-97. doi: 10.1177/1756283X15580743.
Regorafenib (Stivarga, BAY 73-4506; Bayer Pharma AG, Berlin, Germany) is an oral multikinase inhibitor that targets the angiogenic tumor microenvironment and oncogenic kinases including vascular endothelial growth factor receptor 2 (VEGFR2), VEGFR1, VEGFR3, fibroblast growth factor receptor 1 (FGFR1), RAF, KIT, RET and BRAF. Its antiangiogenic effect is greater than that of its related drug, sorafenib. Regorafenib has been approved by the US Food and Drug Administration (FDA) for the treatment of metastatic colorectal cancer (mCRC) in patients who have failed treatment with fluoropyrimidine, oxaliplatin and irinotecan based chemotherapy, an anti-VEGF therapy and, if KRAS wild type, an anti-EGFR therapy. The FDA based this approval on data from the CORRECT trial, which showed the efficacy of regorafenib compared with placebo. The most common grade 3-4 adverse reactions with the drug are hand foot skin reactions (HFSR), diarrhea, hypertension and fatigue. This review discusses the efficacy data, and the incidence and management of regorafenib's toxicities.
瑞戈非尼（拜万戈，BAY 73 - 4506；德国柏林拜耳制药公司）是一种口服多激酶抑制剂，作用于血管生成性肿瘤微环境和致癌激酶，包括血管内皮生长因子受体2（VEGFR2）、VEGFR1、VEGFR3、成纤维细胞生长因子受体1（FGFR1）、RAF、KIT、RET和BRAF。其抗血管生成作用强于相关药物索拉非尼。瑞戈非尼已获美国食品药品监督管理局（FDA）批准，用于治疗经氟嘧啶、奥沙利铂和伊立替康为基础的化疗、抗VEGF治疗失败，且如果KRAS为野生型则经抗EGFR治疗失败的转移性结直肠癌（mCRC）患者。FDA基于CORRECT试验的数据做出这一批准，该试验显示了瑞戈非尼对比安慰剂的疗效。使用该药物最常见的3 - 4级不良反应为手足皮肤反应（HFSR）、腹泻、高血压和疲劳。本综述讨论了瑞戈非尼的疗效数据以及其毒性的发生率和处理方法。
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