Stivarga®(regorafenib，レゴラフェニブ錠）多靶点酪氨酸激酶抑制剂，用于治疗转移性结直肠癌、晚期胃肠间质肿瘤
商標名
Stivarga tablets 40mg
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
構造式
性状
本产品是一种粉末细棕红色或浅白色至浅。
微溶于乙醇（99.5），几乎不溶于水这篇文章。
组成
成分含量
1片，口含（41.49mg作为Regorafenibu水合物）40毫克Regorafenibu。
添加剂
微晶纤维素，交联羧甲基纤维素钠，硬脂酸镁，聚维酮，轻质无水硅酸，三氧化二铁，黄色三氧化二铁，大豆卵磷脂，聚乙二醇4000，部分皂化的聚乙烯醇，滑石粉，氧化钛，氧化
性状
颜色，剂型;
淡红色的椭圆形薄膜衣片
效果或疗效
剂量效应和/或使用的疗效
大肠癌的疗效不可切除的晚期或复发
相关使用说明的效果或疗效
在二线治疗的第一线治疗
1。安全性和有效性尚未确定此药已。
有关既往治疗史的病人，这是问题的两个。
2。临床试验，临床结果了解这种药物的安全性和有效性，并做出选择适应患者的事情。
3。辅助化疗中的安全性和有效性，此药物尚未确立。
用法与用量
通常情况下，口服，每天三个星期作为一个160毫克1 Regorafenibu的成人每天一次，饭后，一个星期的休息时间。我重复这一个周期的管理。另外，也需要根据患者的病情来服用。
药理
1，抗肿瘤作用
在大肠癌来源的肿瘤移植小鼠，Regorafenibu抑制肿瘤的生长，当口服给药时。
2，作用机制
抑制激酶（KIT，RET，RAF-1，BRAF）参与肿瘤的形成（PDGFR，FGFR）和（VEGFR1 ~~ 3，TIE2），肿瘤微环境中肿瘤血管生成Regorafenibu（体外）。的小鼠或大鼠植入肿瘤和抑制肿瘤血管生成，Regorafenibu抑制肿瘤细胞增殖的信号转导通路。
包装
錠剤 PTP包装 28錠（4錠×7）
製造販売元（輸入）
バイエル薬品株式会社
完整资料附件：http://www.info.pmda.go.jp/go/pack/4291029F1028_1_01/
Bayer’s Stivarga® (regorafenib) Tablets Approved by U.S. FDA for Treatment of Metastatic Colorectal Cancer
U.S. Food and Drug Administration (FDA) approved Bayer’s Stivarga® (regorafenib) tablets for the treatment of patients with metastatic colorectal cancer (mCRC) who have been previously treated with currently available therapies (including fluoropyrimidine–, oxaliplatin– and irinotecan–based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy).1 The approval of Stivarga is based on results from the pivotal Phase III study (CORRECT) that demonstrated improvement in overall survival (OS) and progression-free survival (PFS) compared to placebo in patients with mCRC whose disease had progressed after approved standard therapies.2, 3
Stivarga is a Bayer compound developed by Bayer. In 2011, Bayer entered into an agreement with Onyx Pharmaceuticals, Inc. under which Onyx will receive a royalty on any future global net sales of Stivarga in oncology. Bayer and Onyx will jointly promote Stivarga in the United States.
“The approval of regorafenib adds to the treatments we have for metastatic colorectal cancer, which is important for those patients who have no further options,” said Heinz-Josef Lenz, MD, FACP, CORRECT investigator and associate director for clinical research and co-leader of the Gastrointestinal Cancers Program at the USC Norris Comprehensive Cancer Center. “The drug has been shown to prolong survival and slow the progression of cancer in patients whose disease has progressed after treatment with currently available therapies. It provides patients another avenue to fight this cancer.”
In the CORRECT (Colorectal cancer treated with regorafenib or placebo after failure of standard therapy) trial, Stivarga plus best supportive care (BSC) significantly improved OS [HR=0.77 (95% CI, 0.64-0.94), two-sided p=0.0102] and PFS [HR=0.49 (95% CI, 0.42-0.58), two-sided p<0.0001] compared to
