新一代每周口服一次的糖尿病新药Omarigliptin/MK-3102（商品名 Marizev マリゼブ錠）率先获日本批准上市，用于治疗成人2型糖尿病患者 マリゼブ錠１２.５ｍｇ／マリゼブ錠２５ｍｇ 分类名称 可持续性选择性DPP-4抑制剂 ◎口服降糖药◎ 商標名 MARIZEV Tablets 一般名 オマリグリプチン(Omarigliptin) 化学名 (2R ,3S ,5R )-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c ]pyrazol-5(4H )-yl]tetrahydro-2H -pyran-3-amine 分子式 C17H20F2N4O3S 分子量 398.43 性状 本品是一种白色粉末，不吸湿。此产品是易于微溶于乙腈，难溶在甲醇中，微溶于乙酸异丙酯或水。 構造式 条件批准 对制药风险管理计划的发展，要正确实施。 药效药理 1. 作用机序 胰高血糖素样肽1是肠促胰岛素（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP）是参与维持葡萄糖体内平衡的激素。二肽基肽-4（DPP-4）抑制剂，肠降血糖素延迟激素的失活，通过增加活性肠促胰岛素水平，血糖依赖性和增强的胰岛素分泌促进作用和胰高血糖素的浓度降低效果以改善血糖控制。 2. 药理作用 (1) DPP-4抑制活性和活性GLP-1浓度的增加作用 1) Omariguripuchin人DPP-4（重组的，血清衍生）活性选择性抑制在重组DPP-41.6nM的IC 50值，IC 50值的血清衍生的DPP-4是2.1nM（这是2％血清）和6.7nM（50％血清）（体外） 2) 在使用正常小鼠，抑制和活性GLP-1浓度的葡萄糖耐受性试验在等离子体增加血浆中的DPP-4用Omariguripuchin的单次口服给药观察到。 3) Omariguripuchin为25mg在例2型糖尿病患者口服每周一次，共12周施用，后7天最后一次给药的DPP-4活性抑制率分别为82.6％。 (2) 糖耐量和糖代谢的改善作用 1) 12周口服Omariguripuchin为25mg糖尿病患者每周2型时，降低空腹血糖，抑制的降低，观察到餐后高血糖的糖化血红蛋白。 2) 在使用正常小鼠中的葡萄糖耐受性试验，Omariguripuchin通过单次口服给药抑制血糖值的升高。 适应病症 2型糖尿病 用法用量 成年人；一周一次口服给药，每次为25mg 包装规格 片剂： 12.5毫克：PTP 10片（2片板×5） 25毫克：PTP 20片（2片板×10） 制造厂商 MSD有限公司 注：使用以原处方为准：http://www.info.pmda.go.jp/go/pack/3969025F1022_1_05/ Launched once a week, DPP-4 inhibitor "Malisib ®" in Japan ahead of the rest of the world MSD) today announced that it is a sustained selective DPP-4 inhibitor, "Marysb ® tablet 25 mg / 12.5, administered once a week for treatment of type 2 diabetes, headquartered in Chiyoda Ward, Tokyo, President: Tony Alvarez Mg (common name: omagliptin, hereinafter "Maryseb ®") was released. Marijsev ® approval and release are both the world's first. "MALIZEB ®" is a long-acting novel DPP-4 inhibitor developed by Merck & Co., Inc., Kenilworth, N.J., U.S.A. Unlike dosage forms administered once or twice daily, Maryseb controls blood sugar levels with weekly dosing with a characteristic pharmacokinetic mechanism. The domestic Phase III clinical trial confirmed the same efficacy and tolerability as Januvia ® (generic name: sitagliptin), which is a selective DPP - 4 inhibitor administered daily, has been confirmed. Since the effect of "Maryseb ®" is administered once a week for 1 week, it is expected to reduce the patient's burden of medication, motivation to continue therapy and improvement of medication adherence. MSD will provide treatment options to respond to diverse lifestyles of type 2 diabetes patients by adding "Malisib ®" to the diabetes treatment portfolio including Japan's first DPP-4 inhibitor Januvia ® . In addition, we actively take measures to support patients 'continuation of treatment, such as providing new tools to support diabetic patients' diet and exercise therapy and devising product packages to encourage improvement in adherence, We aim to become a true partner in the domain. About MSD MSD is a global healthcare leader who continues to strive to realize a healthy world. MSD is the name used by Merck & Co., Inc., Kenilworth, N.J., U.S.A. in doing business in each country (outside the US and Canada). We cooperate with customers through the provision of medical drugs, vaccines, biopharmaceuticals and animal health products, and we are developing innovative healthcare solutions by developing business in more than 140 countries around the world. Also, through various programs and partnerships, we are actively engaged in activities to promote access to medical care. For more information on MSD please visit www.msd.co.jp.