武田（Takeda）3月7日宣布，已向日本卫生劳动福利部（MHLW）提交了糖尿病新药trelagliptin succinate（曲格列汀琥珀酸盐，开发代码：SYR-472）的新药申请（NDA），该药开发用于2型糖尿病的治疗。
Trelagliptin（曲格列汀）是一种每周一次的二肽基肽酶IV（DPP-4）抑制剂，通过选择性、持续性抑制DPP-4，控制血糖水平。DPP-4是一种酶，能够引发肠促胰岛素（胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP））的失活，而这2种肠降胰岛素在血糖调节中发挥着重要作用。抑制DPP-4，能够增加血糖水平依赖性胰岛素分泌，从而控制血糖水平。
Trelagliptin NDA的提交，是基于在日本2型糖尿病患者中开展的数个III期临床试验的疗效和安全性数据。trelagliptin的疗效在所有试验中均得到了证实，同时具有良好的安全性和耐受性。trelagliptin每周给药1次便可有效控制血糖水平，有望改善患者的用药依从性。
据了解，DPP-4抑制剂是首类可通过提高机体自身能力控制血糖水平的新型2型糖尿病药物，可用作单药，也可与其它口服降糖药联用。其作用机制独特，具有不产生低血糖、不引起体重增加，以及副作用小等独特优势，引起胃肠道不良反应的发生率亦很低。
Osaka, Japan, March 7, 2014 –Takeda Pharmaceutical Company Limited (“Takeda”) announced today that it has submitted a New Drug Application ("NDA") to the Japanese Ministry of Health, Labour and Welfare for trelagliptin succinate (development code: SYR-472), a treatment for type 2 diabetes.
Trelagliptin succinate, discovered by Takeda California, Inc., Takeda's wholly-owned subsidiary located in San Diego, California, is a once-weekly dipeptidyl peptidase-IV (DPP-4) inhibitor. It 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 hormones* 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.
This application is 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 trelagliptin succinate was confirmed in all studies, in addition to a good safety and tolerability profile. Trelagliptin succinate controls blood glucose levels effectively with single weekly dosing, and is expected to contribute to improvement in drug adherence of patients.
We will continue to collaborate closely with the health authorities so that we can provide this new treatment option to meet a variety of needs of patients with type 2 diabetes as well as healthcare providers as soon as possible.
*An insulinotropic gastrointestinal hormone
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