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NESINA(alogliptin benzoate Type,阿格列汀片）

2013-02-01 15:55:32 作者：新特药房来源：互联网浏览次数：593 文字大小：【大】【中】【小】

简介：2013年1月28日,美国食品药品管理局(FDA)最终批准二肽基肽酶Ⅳ(DPP-4)抑制剂阿格列汀上市。 FDA药物评价和研究中心代谢和内分泌部主任Mary Parks，M.D.说：“在糖尿病的总体治疗和护理中控制血糖水平非常 ...

关键字：NESINA(alogliptin benzoate Type 阿格列汀片）二肽基肽酶Ⅳ(DPP-4)抑制剂 2型糖尿病

2013年1月28日,美国食品药品管理局(FDA)最终批准二肽基肽酶Ⅳ(DPP-4)抑制剂阿格列汀上市。
FDA药物评价和研究中心代谢和内分泌部主任Mary Parks，M.D.说：“在糖尿病的总体治疗和护理中控制血糖水平非常重要，”“Alogliptin有助于刺激餐后释放胰岛素，导致更佳控制血糖。
”
批准日期: 1月 25, 2013；公司: 武田制药Takeda Pharmaceutical 公司。

NESINA(alogliptin)片
美国初次批准：2013

一般描述
NESINA片含活性成分alogliptin，是一种选择性，口服生物利用的二肽肽酶-4(DPP-4)酶活性的抑制剂。
化学上，alogliptin被制备为苯甲酸盐，被鉴定为 2-({6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl}methyl)benzonitrile monobenzoate。分子式C18H21N5O2•C7H6O2和分子量461.51道尔顿。结构式为：

Alogliptin苯甲酸盐是白色至淡白色，结晶粉含一个不对称碳在氨基哌啶部分。溶于二甲基亚砜，微溶于水和甲醇及乙醇，和极微溶于辛醇和乙酸异丙酯。
每片NESINA片含34 mg，17 mg，或8.5 mg alogliptin苯甲酸盐分别等同于25 mg，12.5 mg，或6.25 mg， alogliptin和以下无活性成分：甘露醇，微晶纤维素，羟丙基纤维素，交联羧甲基纤维素钠，和硬脂酸镁。此外，包膜衣含以下无活性成分：羟丙甲纤维素，二氧化钛，三氧化二铁(红或黄色)，和聚乙二醇，和被印刷油墨标记(灰F1)。

作用机制
小肠对进餐反应释放肠促胰岛素激素[incretin hormones]例如胰高血糖素-样肽-1(GLP-1)和葡萄糖依赖性促胰岛素多肽[glucose-dependent insulinotropic polypeptide(GIP)]的增加的浓度。这些激素引起胰腺β细胞以葡萄糖依赖方式释放胰岛素，但是这些激素在几分钟内被二肽肽酶-4(DPP-4)失活。GLP-1还减低从胰腺α细胞分泌一改血糖素[glucagon]，减低肝脏葡萄糖生成。在2型糖尿病患者中，GLP-1浓度被减低但保留胰岛素对GLP-1反应。Alogliptin是一种DPP-4抑制剂减慢肠促胰岛素激素的失活，从而在2型糖尿病患者中增加其血流浓度和以葡萄糖依赖方式减低空腹和餐后葡萄糖浓度。在体外在接近治疗性暴露浓度Alogliptin选择性结合至和抑制DPP-4 但不抑制DPP-8或DPP-9 活性。

适应证和用途
NESINA是一种二肽肽酶-4(DPP-4)抑制剂适用为辅助饮食和远动改善血糖控制2型糖尿病成年。(1.1，14)
使用的限制：不是为治疗1型糖尿病或糖尿病酮症酸中毒。(1.2)

剂量和给药方法
（1）正常肾功能或轻度肾受损患者推荐剂量是 25 mg每天1次。 (2.1)
（2）可有或无食物服用。(2.1)
（3）调整剂量如中度或严重肾受损或肾病终末期(ESRD). (2.2)

剂型和规格
片剂
（1）25 mg片是淡红色，椭圆形，双凸，薄膜包衣，一侧印有”TAK ALG-25”。
（2）12.5 mg片是黄色，椭圆形，双凸，薄膜包衣，一侧印有“TAK ALG-12.5”。
（3）6.25 mg片是浅粉色，椭圆形，双凸，薄膜包衣，一侧印有“TAK ALG-6.25”。

禁忌证
对含alogliptin产品，例如过敏性反应，血管水肿或严重皮肤不良反应的严重超敏性反应史。(4)

警告和注意事项
（1）急性胰腺炎：有上市后急性胰腺炎报告。如怀疑胰腺炎，立即终止NESINA。(5.1)
（2）超敏性：在用NESINA治疗患者中有严重超敏性反应上市后报告例如过敏性反应，血管水肿和严重皮肤不良反应。在这类病例中立即终止NESINA，评估其他潜在原因，开始适当监视和治疗，和开始对糖尿病另外治疗。 (5.2)
（3）肝脏影响：肝衰竭上市后报告，有时致命性。不能排除因果关系。如检测到肝损伤，立即中断NESINA和评估患者可能的原因，如可能然后治疗原因，解决或稳定化。如确认肝损伤和不能找到另外病因不要重新开始NESINA。 (5.3)
（4）低血糖：当使用胰岛素促分泌素(如磺酰脲类)或胰岛素与NESINA联合治疗，可能需要较低剂量胰岛素促分泌素或胰岛素以减低低血糖风险。(5.4)
（5）大血管结局：尚无临床研究确定用NESINA或任何其他降糖药大血管风险减低的结论性证据。(5.5)

不良反应
常见不良反应(报道用NESINA 25 mg治疗患者 ≥4%和比接受安慰剂患者更频)是：鼻咽炎，头痛，和上呼吸道感染。 (6.1)
为报告怀疑不良反应，联系Takeda Pharmaceuticals电话1-877-TAKEDA-7(1-877-825-3327)或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.

Launches of “NESINA^®” for treatment of type 2 diabetes, “UNISIA^®” for treatment of hypertension
and “Vectibix^®”, anti-cancer agent, in Japan

OSAKA, Japan, June 15, 2010 --- Takeda Pharmaceutical Company Limited (“Takeda”) today announced that it launched “NESINA^®” (generic name: Alogliptin) for treatment of type 2 diabetes, “UNISIA^®” (generic name: Candesartan Cilexetil / Amlodipine Besilate) for treatment of hypertension and “Vectibix^®” (generic name: Panitumumab), anti-cancer agent.

NESINA is a dipeptidyl peptidase-IV (DPP-4) inhibitor and was created by Takeda San Diego, Inc., Takeda's wholly-owned subsidiary located in San Diego, California. It exhibits extremely high selectivity for DPP-4 inhibition and a once daily dosing with NESINA provides outstanding hypoglycemic benefits. As for indications, it is the only DPP-4 inhibitor that permits combination with alpha-glucosidase inhibitor, which is in common use in Japan.

UNISIA is a fixed dose combination tablet of Blopress^® (generic name: Candesartan Cilexetil) and Amlodipine Besilate (generic name) and they are most prescribed Angiotensin Receptor Blocker (ARB) and Calcium Channel Blocker (CCB) respectively in Japan for treatment of hypertension. A once daily dosing with UNISIA provides outstanding anti-hypertensive benefits. In the guideline 2009 issued by The Japanese Society of Hypertension, the combination therapy of anti-hypertensive treatments is recommended, and the combination of ARB and CCB is one of such treatments in that guideline, being a logical one from the viewpoints of safety and efficacy, without affecting the efficacy of each medicine.

Vectibix was originally developed by Amgen Inc., located in Thousand Oaks, California, and Takeda Bio Development Center Limited^[*], Takeda's wholly-owned subsidiary located in Tokyo, has been conducting the clinical development in Japan. It is an anti-EGFR human monoclonal antibody for treatment of advanced or recurrent colorectal cancer. It binds to epidermal growth factor receptor (EGFR), and suppresses tumor growth. It shows a low incidence of allergic reaction upon and also after administration.

“We are extremely delighted about the launches of these three products,” said Yasuhiko Yamanaka, a member of the board, senior vice president, Pharmaceutical Marketing Division of Takeda. “We expect that NESINA and UNISIA will help us to further drive our Metabolic & Cardiovascular franchise, where we currently have the edge. Our plan is to maximize the potential of our line in this strategic area. Having multiple drugs with different mechanisms of action will allow us to propose treatments that best match the conditions of individual patients. Meanwhile, through the promotion of Vectibix we wish to contribute to the treatment of colon cancer patients, thus making it a springboard for our full-fledged challenge to become a leader in the oncology area.”

The combined sales of these three products (at NHI price basis) are estimated around 10 billion yen. Takeda intends to make these three the future mainstay products that will drive its performance in Japan, by providing scientific information to as many healthcare professionals as possible.

^[*]It is in charge of development of Takeda’ s oncology products in Japan

<Reference>

Brand Name NESINA® Tablets 25mg, 12.5mg & 6.25mg

Generic Name Alogliptin Benzoate

Dosage and Usage NESINA is orally administered to adults once daily as Alogliptin 25mg.

Indications Type 2 Diabetes
In patients inadequately glycemic controlled by following treatments,
1. Treatment by diet and exercise only
2. In addition to treatment by diet and exercise, treatment by alpha-glucosidase inhibitor

Product registration Approved on April 16, 2010

alogliptin：老年用药更安全有效

日前在《美国老年医学会杂志》上刊登的一篇文章报道，二肽基肽酶-4（DPP-4）抑制剂alogliptin对于治疗2型糖尿病的老年患者既安全又有效。美国佛蒙特大学Richard博士说：“DPP-4抑制剂对于老年糖尿病患者十分有效，且具有很好的可耐受性，因此，可以用其来代替磺脲类药物。”
Richard博士及其研究小组通过对455名2型糖尿病老年患者和1911名年轻患者进行研究，分析alogliptin的有效性、安全性和可耐受性。结果发现，无论年龄大小，alogliptin的给予剂量为12.5mg或25mg时，均可有效地降低HbA1c水平。当HbA1c的基准线为8.0％甚至更低时，老年患者的HbA1c下降的比例较年轻患者多；如果基准线定为8.0％以上时，则两组研究对象的HbA1c下降比例基本相同。该研究忽略了所有研究对象的体重变化，并且经检测两组受试人群脂质结果的差异不明显。
Richard博士说：“在治疗2型糖尿病老年患者时，应该将DPP-4抑制剂替代磺脲类药物，或者作为二甲双胍的添加剂，用于可以耐受二甲双胍治疗和肾功能良好的患者，而对于不能耐受二甲双胍或肾功能不良的患者，alogliptin应成为优先考虑的治疗方法。

「ネシーナ錠６・２５mg、同１２・５mg、同２５mg」は、武田サンディエゴが創製した１日１回投与のＤＰＰ‐４阻害剤。ＤＰＰ‐４に対する選択性が高く、単剤・α‐グルコシダーゼ阻害剤との併用で投与される。

医薬品名:ネシーナ錠6.25mg
一般名:アログリプチン安息香酸塩

医薬品名:ネシーナ錠12.5mg
一般名:アログリプチン安息香酸塩

医薬品名:ネシーナ錠25mg
一般名:アログリプチン安息香酸塩