英文药名：Stivarga tablets(Regorafenib Hydrate) 中文药名：盐酸瑞格非尼片 生产厂家：拜耳制药 スチバーガ錠40mg 药物分类名称 抗肿瘤药/激酶抑制剂 批准日期：2013年5月 商標名 Stivarga tablets 40mg 構造式 一般名 レゴラフェニブ水和物（Regorafenib Hydrate）JAN （regorafenib）INN 化学名 4-［4-（｛［4-Chloro-3-（trifluoromethyl）phenyl］carbamoyl｝amino）-3-fluorophenoxy］-N-methylpyridine-2-carboxamide monohydrate 分子式 C21H15ClF4N4O3・H2O 分子量 500.83 性状 该产品为白色至略带淡红色或三色粉末。 该产品难溶于乙醇（99.5），几乎不溶于水。 批准条件 制定药品风险管理计划并适当实施。 药用药理学 1.抗肿瘤作用 Legolafenib通过口服给予移植结肠/直肠癌和胃肠道间质肿瘤衍生肿瘤的小鼠抑制肿瘤生长，并通过口服给予移植源自肝细胞癌的肿瘤的小鼠提高存活率 我做到了。 2.作用机制 Legolafenib抑制参与肿瘤血管生成（VEGFR1-3，TIE2），肿瘤微环境（PDGFR，FGFR）和肿瘤发生（KIT，RET，RAF-1，BRAF）（体外）的激酶。 此外，它抑制突变体KIT（V560G，V654A，D816H，D820Y和N822K突变）的活性（体外）。Legolafenib抑制肿瘤血管生成并抑制肿瘤移植的小鼠或大鼠中肿瘤细胞增殖的信号传导途径。 适应症 癌症化疗后无法切除的可治愈的肝细胞癌，癌症化疗后无法切除的可治愈的胃肠道间质瘤的进展/复发的结直肠癌 用法与用量 成年，每天一次160毫克，每天在饭后口服三周，持续一周，然后休息一周。 以此为循环重复给药。另外，根据患者的状况进行减重。 包装 片剂 PTP：28粒（4片×7）/包装 制造商销售代理（进口） 拜耳制药有限公司 注：以上中文资料不够完整，使用者以原处方资料为准。 完整说明资料附件：http://www.info.pmda.go.jp/go/pack/4291029F1028_1_09/ Stivarga(regorafenib, anthraquinone)multi-target tyrosine kinase inhibitor for the treatment of metastatic colorectal cancer, advanced gastrointestinal stromal tumors On August 20, 2013, Bayer announced today that the new indication for oral multi-kinase inhibitor Stivarga (regorafenib) has been approved by the Ministry of Health, Labor and Welfare (MHLW) for systemic cancer therapy. Treatment of patients with gastrointestinal stromal tumors (GIST) with worsening condition. This is the second indication that Stivarga was approved in Japan. The approval of the new indication for Stivarga is based on the results of a critical phase III GRID trial. The data showed that Stivarga significantly improved disease compared with placebo in patients with GIST who had been worsened after treatment with imatinib mesylate and sunitinib malate. Progressive life (PFS). Data from the GRID study was presented to the American Society of Clinical Oncology (ASCO) meeting in June 2012 and published online November 22, 2012, The Lancet. Currently, Stivarga has been approved by several countries including the United States and Japan for the treatment of patients with metastatic colorectal cancer (mCRC). The drug was approved by the European Medicines Agency (EMA) Human Pharmaceutical Products Committee (CHMP) on June 27, 2013, and recommended approval for the treatment of adult patients with mCRC. The European Commission (EC) is expected to be later in 2013. Time to make an approval decision. On February 25, 2013, the FDA approved a new Stivarga indication for the treatment of patients with GIST who had been previously treated with other kinase inhibitors (Gleevec, Sutent) or who were unable to undergo surgical resection. Stivarga is the third FDA-approved drug for the treatment of gastrointestinal stromal tumors. The other two are Novartis's Gleevec and Pfizer's Sutent. Developed by Bayer, Stivarga was jointly promoted by Bayer and Onyx Pharmaceuticals and was approved for mCRC treatment in September 2012. Gastrointestinal stromal tumor (GIST) is a tumor in which the cancer cells occur in the gastrointestinal tract. Most of the patients are elderly. Stivarga is an oral multi-kinase inhibitor that inhibits several pro-angiogenic VEGF receptor tyrosine kinases in preclinical studies. These kinases play an important role in tumor angiogenesis. The drug also inhibits multiple kinases in cancer and tumor microenvironments, including VEGFR 1-3, KIT, RET, PDGFR and FGFR.