2016年10月8日，宣布，日本卫生劳动福利部（MHLW）已批准糖尿病复方新药Alogliptin Benzoate/Metformin Hydrochloride（商标名 INISYNC Combination Tablets 武田研发），用于2型糖尿病的治疗。Inisync复方片由固定剂量的Nesina（阿格列汀，alogliptin，25mg）和二甲双胍（500mg）组成，每日口服一次。此次批准，使Inisync成为日本市场唯一一种每日口服一次的DPP-4和二甲双胍复方药。   Inisync的获批，是基于与Nesina相关的现有临床数据以及在日本开展的Inisync的III期临床研究。所有这些临床试验均调查了Nesina和二甲双胍联合用药的疗效和安全性。来自III期临床的数据显示，与Nesina单药治疗和二甲双胍单药治疗相比，Nesina+二甲双胍同时用药（每日一次）使糖化血红蛋白（HbA1c）实现了显著更大幅度的降低，达到了研究的主要终点。研究中，Nesina和二甲双胍同时用药的安全性与2种药物单独用药的安全性一致。   Nesina是一种口服二肽基肽酶-4抑制剂（DPP-4i），可减缓肠促胰岛素激素（incretin hormones）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，从而增加活性肠促胰岛素的总量，使胰脏以一种葡萄糖依赖的方式分泌胰岛素，协助管理血糖水平。   二甲双胍则是一种双胍类药物，常用作2型糖尿病早期治疗的一线药物，可单独或与其他药物（包括胰岛素）联合用药。在2型糖尿病患者中，肝脏产生过量的葡萄糖（glucose），从而推高血糖水平。二甲双胍可通过降低肝脏产生葡萄糖的量、增加肌肉对葡萄糖的敏感性、延缓肠道的葡萄糖吸收，降低机体的血糖水平。具有机制互补和协同增效作用，将为广大2型糖尿病群体提供一种更有效的治疗选择。 附：原研处方资料：http://www.info.pmda.go.jp/go/pack/3969105F1023_1_04/ Takeda Obtains New Drug Application Approval for Inisync® Combination Tablets for the Treatment of Type 2 Diabetes in Japan Takeda Pharmaceutical Company Limited (TSE: 4502) today announced that Takeda has obtained the New Drug Application Approval from the Ministry of Health, Labour and Welfare for the Inisync® Combination Tablets, a fixed-dose combination of Nesina® (generic name: alogliptin benzoate) and metformin hydrochloride (hereinafter “metformin”) for the treatment of type 2 diabetes. Inisync combination tablets combine 25 mg Nesina and 500 mg metformin, which is orally administered once daily. Nesina is a once-daily dipeptidyl peptidase-IV (DPP-4) inhibitor, and metformin is biguanide that inhibits sugar production in the liver administered twice or three times daily. Both of them are widely used as therapeutic drugs for the treatment of diabetes. Inisync is the only combination tablets administered once daily of a DPP-4 inhibitor and metformin in Japan. The approval is based on the results of the existing clinical studies related to Nesina and the Phase III study for Inisync in Japan. In all studies, the efficacy and safety have been investigated for the ingredients of this combination tablets, Nesina and metformin, when they are concomitantly administered. The results of the Phase III study have shown significantly higher effects in improving HbA1c in regards to the changes in HbA1c, the primary endpoint, when Nesina and metformin are concomitantly administered once daily compared to individual administration of Nesina or metformin. It has also been confirmed that the safety and the tolerance were equal in the concomitant intake compared to the individual administration of Nesina only or metformin only. “The number of patients with type 2 diabetes is increasing every year, but for various reasons, there are many patients who discontinue their diabetes treatment.” said Emiko Koumura,　M.D., Ph.D., Senior Director of Clinical Science, Takeda Development Center Japan. “We have various therapeutic options for the treatment of type 2 diabetes, and we have been providing therapeutic options based on the needs of medical professionals as well as of individual patients. I expect that this combination will contribute to improvement in treatment adherence for patients with type 2 diabetes, and to continue their therapies by providing new options for their treatment.” *ADPP-4 inhibitor enhances the insulin secretion based on the plasma glucose levels, and it controls the levels by selectively inhibiting DPP-4 activity that inactivates two hormones, the incretin hormones (gastrointestinal hormones that promote insulin secretion) that play important roles in adjusting blood glucose, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) <About Inisync Combination Tablets> Name of the product Inisync® Combination Tablets Generic Name Alogliptin benzoate and metformin hydrochloride Indication Type 2 diabetes However, administration is limited only when it is judged appropriate to treat it concomitantly with alogliptin benzoate and metformin hydrochloride. Dosage and administration Usually, for adults, one tablet (25 mg/500mg as alogliptin benzoate/metformin hydrochloride) is orally administered once daily immediately before meals or after meals. About Takeda’s Diabetes Business Takeda’s heritage in diabetes globally includes significant contributions towards scientific discovery and exchange, starting with the discovery of the thiazolidinedione (TZD) pioglitazone, the more recent developments of alogliptin and the fixed-dose combinations (FDC) alogliptin and pioglitazone, and alogliptin and metformin HCl. The company’s diverse diabetes portfolio show Takeda’s ongoing commitment to advancing patient care and helping to meet the individual needs of this growing patient population. About Takeda Pharmaceutical Company Takeda Pharmaceutical Company Limited is a global, research and development-driven pharmaceutical company committed to bringing better health and a brighter future to patients by translating science into life-changing medicines. Takeda focuses its R&D efforts on oncology, gastroenterology and central nervous system therapeutic areas plus vaccines. Takeda conducts R&D both internally and with partners to stay at the leading edge of innovation. New innovative products, especially in oncology and gastroenterology, as well as our presence in Emerging Markets, fuel the growth of Takeda. More than 30,000 Takeda employees are committed to improving quality of life for patients, working with our partners in health care in more than 70 countries.