英文药名：XELJANZ Tablets（Tofacitinib Citrate） 中文药名：柠檬酸托法替尼片 生产厂家：辉瑞制药 ゼルヤンツ錠5mg Xeljanz为一种Janus激酶（JAK）抑制剂，是日本获批的首个JAK抑制剂类口服RA药物。与生物制剂靶向于胞外细胞因子不同，Xeljanz靶向于JAK通路，该信号通路在RA炎症中发挥了关键作用。 Xeljanz可用于经至少一种疾病修饰抗风湿药物（DMARD，如氨甲喋呤）治疗后仍存在临床症状的患者。Xeljanz获批的剂量为5mg，每天2次。 治疗类别名称 Janus激酶（JAK）抑制剂 批准上市：2013年5月 商標名 XELJANZ Tablets 一般名 トファシチニブクエン酸塩（Tofacitinib Citrate） 化学名 3-｛（3R,4R）-4-Methyl-3-［methyl（7H-pyrrolo［2,3-d］pyrimidin-4-yl）amino］piperidin-1-yl｝-3-oxopropanenitrile monocitrate 分子式 C16H20N6O・C6H8O7 分子量 504.49 構造式 性状 本品是一种白色粉末。此产品是N，N-二甲基乙酰胺更可溶，微溶于水，乙醇（99.5）非常微溶。 条件批准 1.上市后，直至有关一定数量的案件数据积累，通过开展对一切案件的表现使用调查，收集有关这种药物的早期安全性和有效性数据然后，采取必要的措施，正确使用此药。 2.实施适当的上市后监测，并仔细考虑这种药物的安全，要考虑安全性和有效性在长期服用的时间，包括这些感染的表达。 药效药理 作用机序 TOFACITINIB是JAK家族的有效抑制剂，它显示了在人类中的激酶中的高选择性。 TOFACITINIB是激酶测定抑制JAK1，JAK2，JAK3，也抑制轻度TYK2。虽然在细胞JAK两分子进行是信号转导介导的TOFACITINIB有力地由异二聚体受体抑制信号转导即与在JAK2满足JAK3或JAK1，功能选择性联营比的信号转导由同二聚体受体的抑制作用更高。 JAK1和JAK3，IL-2，IL-4，IL-7，IL-9，通过细胞因子受体与几种常见γ链，包括IL-15和信号的IL-21被阻塞的抑制是的。这些细胞因子，淋巴细胞的活化，因为它是对生长和功能性表达必需被认为是由于这些信号传导的抑制可以抑制各种形式的免疫反应。另外，在JAKl的抑制作用，也被认为抑制通过其他促炎性细胞因子如IL-6或I型IFN信号。在较高剂量，存在通过抑制变速器的促红细胞生成素的信号的JAK2同二聚体信号抑制发生的可能性。 适应病症 适用于治疗中度至严重活动性类风湿性关节炎成年患者对氨甲喋呤已反应不佳或不能耐受。 用法与用量 成人；每日口服二次，每次为5毫克。 包装规格 ゼルヤンツ錠5mg：28錠（PTP） 制造商 辉瑞日本公司 完整资料附件： http://www.info.pmda.go.jp/go/pack/3999034F1020_1_05/ New oral rheumatoid arthritis remedy New release of JAK inhibitor "ZERYZZ ® tablet 5 mg" - New options for treatment of rheumatoid arthritis, regarding promotion of proper use - Takeda Pharmaceutical Co., Ltd. (Headquarters: Chuo Ward, Osaka-shi, hereinafter referred to as "Takeda Pharmaceutical"), on July 30, 2013, "Pfizer Inc. (head office: Shibuya- "(Generic name: tofacitinib citrate, hereinafter" ZERYZ ") will be released. As a treatment for rheumatoid arthritis in adults with insufficient efficacy with existing treatments, this product was approved by the Ministry of Health, Labor and Welfare on March 25, 2013, and was listed on the drug price on May 24. Pfizer and Takeda Pharmaceutical will sell this product under co-promotion as well as Enbrel (generic name: Etanercept) for treating rheumatoid arthritis. Zeruzants is the first oral treatment for oral rheumatoid arthritis approved in Japan as a new drug class called JAK (Janus Kinase) inhibitor. Ezetimibe targets intracellular signaling that plays an important role in inflammation associated with rheumatoid arthritis, unlike biologics that target cytokines to the outside of the cell, and its pathway JAK (Janus Kinase) Pathway It inhibits. In past therapy, Zeruzantz is usually treated with at least one antirheumatic drug (DMARD) such as methotrexate or the like, but if clear symptoms due to the disease remain, it is usually 5 mg once a day It is administered orally twice a day. Pfizer and Takeda Pharmaceutical Co., Ltd., for the safer and more effective use of Zerjantz, the Japanese Rheumatology AssociationUnder the cooperation, in accordance with Tohasitinib usage guidelines of the Japanese Rheumatology Association, we will conduct a survey of all cases after marketing and promote appropriate use. In the guideline, patients with poor control are recommended for treatment by ZERYZZ even if treatment with methotrexate exceeding 8mg/week continues for more than 3 months. We conduct a case study of 4,000 patients under treatment by ZERYZZ for 3 years of observation period and collect and verify safety and efficacy information. In addition, a control group (2,000 patients) who started drug therapy other than bevacizumab is set up and a comparative study will be conducted on malignant tumors and severe infectious diseases. Professor Yoshiya Tanaka, Professor of Internal Medicine, University of Occupational and Environmental Health, Professor Yoshiya Tanaka says, "Rheumatoid arthritis is a serious disease accompanied with physical disorder, some patients can not obtain sufficient effects with existing therapeutic agents, We expect that the appearance of drugs will lead to an improvement in patients' quality of life.Seljants with a new mechanism of action has been evaluated for safety and efficacy in clinical trials both in Japan and overseas, I think that it is important to encourage the proper use of drugs and to build up evidence at clinical workplaces. " Outline of Zeljants® Product name Zeljants ® tablet 5 mg (XELJANZ® Tablets 5 mg) Common name Tofacitinib citrate (Tofacitinib Citrate) Manufacturing marketing approval acquisition date March 25, 2013 Drug price listing date May 24, 2013 Release date July 30, 2013 Manufacturer Distributor Pfizer Inc. Sales Takeda Pharmaceutical Co., Ltd. Indications and efficacies Rheumatoid arthritis inadequate for existing treatments [Usage notes related to indication/effect] In past treatments, even if adequate treatment with at least one antirheumatic drug such as methotrexate is performed, it is administered when obvious symptoms due to disease remain. Dosage/dose Ordinarily, 5 mg once a day as tofacitinib is administered once a day. Characteristic 1. The world's first Janus kinase (JAK) inhibitor in rheumatoid arthritis. 2. New mechanism of action focusing on intracellular signal transduction. It inhibits intracellular signaling by cytokines that utilize JAK Pathway. 3. Molecular targeted therapeutic agent of low molecular weight, achieving oral administration. It shows the improvement effect of symptoms and signs of rheumatoid arthritis by oral administration twice a day. About rheumatoid arthritis Rheumatoid arthritis is a chronic inflammatory autoimmune disease and its symptoms are typically manifested in the hands and feet, but there is a possibility that any joints with synovium may develop. Rheumatoid arthritis suffers from about 70 to 800 thousand people in Japan and about 23.7 million people worldwide. Although there are several existing treatments, there are not a few patients whose treatment effect is not sufficient. Indeed, one-third of patients do not respond adequately, about half will not respond to a specific DMARD within 5 years 3, 4, 5, 6, 7, 8. There is still a desire for further therapeutic drugs to emerge. -------------------------------------------- 产地国家：日本 原产地英文商品名: XELJANZ tab（ゼルヤンツ錠）5mg/tab 28tabs/box  原产地英文药品名: tofacitinib 中文参考商品译名: XELJANZ片（ゼルヤンツ錠）5毫克/片 28片/盒 中文参考药品译名: 枸橼酸托法替尼 生产厂家中文参考译名: 辉瑞 生产厂家英文名: Pfizer ---------------------------------------------- 产地国家: 美国 原产地英文商品名: XELJANZ 5 MG TABLET 60 Tablets 原产地英文药品名: TOFACITINIB CITRATE 中文参考商品译名: XELJANZ 5毫克/片 60片/瓶 中文参考药品译名: 托法替尼 生产厂家中文参考译名: 辉瑞 生产厂家英文名: Pfizer