部份中文瑞格非尼处方资料（仅供参考）
商品名：Stivarga tablets
英文名：Regorafenib
中文名：盐酸瑞格非尼片
生产商：拜尔制药
药品简介 Stivarga（Regorafenib Hydrate，瑞戈非尼片）是一种新型口服多激酶抑制剂，用于转移性结直肠癌（CRC）、胃肠道间质瘤（GIST）及肝细胞癌（HCC）患者的治疗。该药已在美国、欧盟、日本等90多个国家和地区批准使用，于2017年3月24日获CFDA批准上市许可，用于转移性结直肠癌和胃肠道间质瘤患者的治疗。 スチバーガ錠40mg
药物分类名称
抗肿瘤剂/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
本品为白色至淡红色或三色粉末。
该产品难溶于乙醇（99.5），难溶于水。
审批条件
制定药品风险管理计划并适当执行。
药效药理
1.抗肿瘤作用
利拉非尼通过口服施用于移植结肠/直肠癌和胃肠道间质肿瘤衍生的肿瘤的小鼠中抑制肿瘤生长，并通过口服施用给移植了来自肝细胞癌的肿瘤的小鼠提高存活率。
2. 作用机序
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）中的激酶。 此外，它抑制突变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植入小鼠或大鼠中肿瘤细胞增殖的信号传导途径。
适应症
不可切除的晚期/复发性大肠癌
癌症化疗后胃肠道间质瘤恶化
癌症化疗后无法切除的肝细胞癌恶化
用法与用量
通常，对于成年人，饭后连续3天每天口服一次160mg瑞戈非尼，然后休息1周。 设置为一个周期，重复给药。 可以根据患者的病情降低剂量。
包装规格
PTP包装：28片（4片×7）
制造商销售代理（进口）
拜耳药业有限公司
注：以上中文资料不够完整，使用者以原处方资料为准。
完整说明附件： https://www.info.pmda.go.jp/go/pack/4291029F1028_1_10/?view=frame&style=XML&lang=ja
Stivarga(Regorafenib Hydrate tablets) is a good news for patients with metastatic colorectal cancer, gastrointestinal stromal tumor (GIST) and hepatocellular carcinoma (HCC)
Stivarga tablet (Stivarga) is a new type of oral multikinase inhibitor for the treatment of patients with metastatic colorectal cancer (CRC), gastrointestinal stromal tumor (GIST) and hepatocellular carcinoma (HCC). The drug has been approved for use in more than 90 countries and regions including the United States, the European Union, and Japan. It was approved for marketing by the CFDA on March 24, 2017 for the treatment of patients with metastatic colorectal cancer and gastrointestinal stromal tumors.
Colorectal cancer is one of the most common malignant tumors of the digestive tract, and its incidence ranks third among malignant tumors, with 1.36 million new cases each year. According to China's cancer statistics in 2015, the incidence and mortality of colorectal cancer in my country rank among the top five among all malignant tumors. Among them, 37.6/100,000 new cases and 19.1/100,000 deaths are among the highest in my country. The incidence of rectal cancer is on the rise. Studies have shown that if untreated, the median survival time of metastatic colorectal cancer is only 8 months.
Gastrointestinal stromal tumor is the most common form of sarcoma, which originates in the mesenchymal tissue of the gastrointestinal tract. If the disease spreads to other parts of the body (metastasis) or cannot be surgically removed for the purpose of curing, GIST is a life-threatening malignant disease. The incidence of GIST is approximately 11-20 patients/1 million people/year.
Hepatocellular carcinoma is the most common type of liver cancer. About 70-85% of liver cancer cases worldwide are hepatocellular carcinoma. The incidence of liver cancer is increasing worldwide. It is the sixth most common cancer in the world and the second leading type of cancer death. China is a country with a high incidence of hepatocellular carcinoma, and there is still a lack of effective drugs. If Stivarga is approved, it will be expected to benefit these cancer patients.
