以下资料仅供参考

药品使用说明书

英文药名：Zafatek(Trelagliptin succinate Tablets)

中文药名：琥珀酸曲格列汀片

生产厂家：武田制药

治疗类别名称
可持续性选择性DPP-4抑制剂
-2型糖尿病治疗药物-
上市时间：2015年3月7日（日本）
商標名
Zafatek Tablets
化学構造式

一般名 
トレラグリプチンコハク酸塩（Trelagliptin Succinate）〔JAN〕
化学名
2-（｛6-［（3R）-3-Aminopiperidin-1-yl］-3-methyl-2, 4-dioxo-3, 4- dihydropyrimidin -1（2H）-yl} methyl）-4-fluorobenzonitrile monosuccinate
分子式
C18H20FN5O2・C4H6O4
分子量
475.47
融点
187.1℃
性状 
Zafatek是一种白色或类白色结晶或结晶性粉末。水或易溶于二甲基亚砜，难溶于甲醇，乙醇（99.5），微溶于四氢呋喃或二乙胺，在乙腈或2-丙醇非常微溶。
条件批准
在建立药品风险管理计划的顶部，要正确实施。

药效药理
1. 作用机序
通过这种药物以抑制二肽基肽-4（DPP-4）灭活从肠道分泌的胰高血糖素样肽进入血液通过口服摄取刺激选项-1（GLP-1），GLP的活性-1的血液水平升高促进从糖浓度依赖性的胰腺胰岛素分泌。
2. 药理作用
(1) DPP-4抑制效果
1) 选择性抑制人血浆DPP-4活性（IC 50值：4.2nmol/L）体外。此外，为了比较Toreraguripuchin和阿格列汀的DPP-4抑制活性，比较在相同的条件（体外）下的IC 50值和（纳摩尔/升），分别为1.3和5.3。
2) 饮食，运动疗法之间为100毫克作为Toreraguripuchin的12周口服给药用于治疗2型糖尿病也血糖控制不充分进行（一周一次早餐前）为安慰剂对照，双盲，平行组比较研究在，在最后一次给药的平均值7天DPP-4活性抑制率后是Toreraguripuchin100毫克组中的77.4％。
(2) 活性GLP-1浓度的增加作用
饮食，运动疗法之间为100毫克作为Toreraguripuchin的12周口服给药用于治疗2型糖尿病也血糖控制不充分进行（一周一次早餐前）为安慰剂对照，双盲，平行组比较研究在，在12个星期后，膳食耐受性测试活性GLP-1浓度被显著增加相比，安慰剂组为。
(3) 耐糖能改善作用
和Toreraguripuchin的单剂量口服过夜禁食肥胖2型糖尿病模型（威斯特肥鼠）和非肥胖2型糖尿病模型（N- STZ-1.5只大鼠），葡萄糖耐受性试验，其葡萄糖施用后口服给药1小时在葡萄糖耐受性的改善作用进行了观察。
适应病症

用于2型糖尿病的治疗
用法用量
口服，每周一次，每次100mg
包装规格
片剂
50毫克： 20片（2片板×10）

100毫克：20片（2片板×10）

製造販売元 
武田薬品工業株式会社
完整处方附件：http://www.info.pmda.go.jp/go/pack/3969024F1028_1_03/

ZAFATEK® Now Available for the Treatment of Type 2 Diabetes in Japan
Important New Treatment Option is First Once Weekly Oral Option for Type 2 Diabetes Patients
2015–Takeda Pharmaceutical Company Limited (“Takeda”) announced today that ZAFATEK® (generic name: trelagliptin succinate, hereafter “ZAFATEK”) is now available in Japan.
ZAFATEK is a once-weekly oral dipeptidyl peptidase-IV (DPP-4) inhibitor.
ZAFATEK controls blood glucose levels by selectively and continually inhibiting DPP-4, an enzyme that causes the inactivation of glucagon-like peptide-1 and glucagon-dependent insulinotropic polypeptide, incretin hormones1 that play an important role in blood glucose regulation. The inhibition of DPP-4 increases insulin secretion depending on blood glucose concentration, thereby controlling blood glucose levels.
The approval of ZAFATEK was granted based on the safety and efficacy results of multiple clinical phase III studies in patients with type 2 diabetes in Japan. The efficacy of once-weekly ZAFATEK was confirmed in all studies, in addition to an acceptable safety and tolerability profile.
The prevalence of diabetes patients in Japan remains at a high level. According to the National Health and Nutrition Survey of 20122, it is estimated that there are 9.5 million people who are strongly suspected to have diabetes and 11 million people with a high possibility of having diabetes. Medication regimens for patients with type 2 diabetes are complicated and often require them to take their medicine several times a day. ZAFATEK can help patients reduce this burden by controlling blood glucose levels with convenient once-weekly dosing, contributing to improved drug adherence3.
"By adding ZAFATEK as an important new treatment option to our diabetes portfolio in Japan, we believe we are providing more suitable treatment options for the each patient's individual needs," said Masato Iwasaki, Ph.D., Director and President, Japan Pharma Business Unit of Takeda. “ZAFATEK is the world's first once weekly oral type 2 diabetes treatment option. By delivering adequate information to doctors and healthcare providers, we hope ZAFATEK becomes an important therapeutic option for patients.”
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