阿洛利停片|NESINA® (alogliptin benzoate Type)
日本批准武田制药生产的DPP-4抑制剂Alogliptin与噻唑烷二酮类合用治疗2型糖尿病
日本武田制药有限公司（Takeda Pharmaceutical Company Limited）宣称，日本药监部门（Japanese Ministry of Health, Labour and Welfare）已批准其全资子公司武田圣地亚哥公司（Takeda San Diego,Inc.）生产的二肽基肽酶-4（dipeptidyl peptidase-IV，DPP-4）抑制剂Alogliptin（商品名：Nesina）与噻唑烷二酮类（thiazolidinediones）合用治疗2型糖尿病（type 2 diabetes）。
Alogliptin高度选择性地显著抑制DPP-4，延缓胰高血糖素样肽-1（glucagon-like peptide-1，GLP-1）的灭活。GLP-1有助于改善胰岛β细胞功能，增加胰岛素分泌，而噻唑烷二酮类降糖药可减轻胰岛素抵抗。2型糖尿病2个最基本的病理变化就是胰岛素抵抗和胰岛素分泌减少及其分泌节律异常，上述两药合用可从不同环节改善血糖控制，有助于将血糖降至理想水平。
到目前为止，Alogliptin可用于下列血糖控制不好的2型糖尿病患者：单纯饮食和运动疗法治疗者，可单独使用Alogliptin；饮食和运动疗法及α-葡萄糖苷酶抑制剂（α-glucosidase inhibitor）或噻唑烷二酮类治疗者，可加用Alogliptin。Aloglitpin每天口服1次，每次25毫克。具体到每个患者，应遵医嘱。

NESINA® alogliptin benzoate Type 2 diabetes
日本武田制药有限公司（Takeda Pharmaceutical Company Limited）宣称，日本药监部门（Japanese Ministry of Health, Labour and Welfare）已批准其全资子公司武田圣地亚哥公司（Takeda San Diego,Inc.）生产的二肽基肽酶-4（dipeptidyl peptidase-IV，DPP-4）抑制剂Alogliptin（商品名：Nesina）与噻唑烷二酮类（thiazolidinediones）合用治疗2型糖尿病（type 2 diabetes）。
Alogliptin高度选择性地显著抑制DPP-4，延缓胰高血糖素样肽-1（glucagon-like peptide-1，GLP-1）的灭活。GLP-1有助于改善胰岛β细胞功能，增加胰岛素分泌，而噻唑烷二酮类降糖药可减轻胰岛素抵抗。2型糖尿病2个最基本的病理变化就是胰岛素抵抗和胰岛素分泌减少及其分泌节律异常，上述两药合用可从不同环节改善血糖控制，有助于将血糖降至理想水平。
到目前为止，Alogliptin可用于下列血糖控制不好的2型糖尿病患者：单纯饮食和运动疗法治疗者，可单独使用Alogliptin；饮食和运动疗法及α-葡萄糖苷酶抑制剂（α-glucosidase inhibitor）或噻唑烷二酮类治疗者，可加用Alogliptin。Aloglitpin每天口服1次，每次25毫克。具体到每个患者，应遵医嘱。

产品规格；

NESINA(ネシーナ) 6.25毫克/片 100片/盒
NESINA(ネシーナ) 12.5毫克/片 100片/盒
NESINA(ネシーナ) 25毫克/片 100片/盒

ネシーナ錠25mg／ネシーナ錠12.5mg／ネシーナ錠6.25mg

一般名

アログリプチン安息香酸塩（Alogliptin Benzoate）〔JAN〕

化学名

2-（｛6-［（3R）-3-Aminopiperidin-1-yl］-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1（2H）-yl｝methyl）benzonitrile monobenzoate

 

化学構造式

分子式

C₁₈H₂₁N₅O₂・C₇H₆O₂

分子量

461.51

融点

182.5℃

性状

アログリプチン安息香酸塩は白色～帯黄白色の結晶性の粉末である。ジメチルスルホキシドにやや溶けやすく、水又はメタノールにやや溶けにくく、アセトニトリル又はエタノール（99.5）に溶けにくい。

効能又は効果

2型糖尿病

ただし、下記のいずれかの治療で十分な効果が得られない場合に限る。

(1)

食事療法、運動療法のみ

(2)

食事療法、運動療法に加えてα-グルコシダーゼ阻害剤を使用

(3)

食事療法、運動療法に加えてチアゾリジン系薬剤を使用

(4)

食事療法、運動療法に加えてスルホニルウレア系薬剤を使用

(5)

食事療法、運動療法に加えてビグアナイド系薬剤を使用

効能又は効果に関連する使用上の注意

糖尿病の診断が確立した患者に対してのみ適用を考慮すること。糖尿病以外にも耐糖能異常・尿糖陽性等、糖尿病類似の症状(腎性糖尿、甲状腺機能異常等)を有する疾患があることに留意すること。

用法及び用量

通常、成人にはアログリプチンとして25mgを1日1回経口投与する。

用法及び用量に関連する使用上の注意

中等度以上の腎機能障害患者では、排泄の遅延により本剤の血中濃度が上昇するため、腎機能の程度に応じて、投与量を適宜減量すること。（【薬物動態】の項参照）

 

包装

ネシーナ錠25mg

ネシーナ錠12.5mg

ネシーナ錠6.5mg

「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

メーカー:武田薬品
販売:武田薬

Launches of “NESINA®” for treatment of type 2 diabetes, “UNISIA®” for treatment of hypertensionand “Vectibix®”, anti-cancer agent, in JapanOSAKA, 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.

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