美国FDA于2011年5月2日批准Tradjenta片剂(有效成分为linagliptin)治疗成人2型糖尿病,主要用于结合饮食和运动改善病人对血糖水平的控制。胰岛素是一种调节血糖水平的激素,而2型糖尿病患者主要是由于自身不能产生胰岛素或者对胰岛素无正常反应。
TRADJENTA - linagliptin片剂，薄膜包衣
勃林格殷格翰制药公司
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Tradjenta™（linagliptin）片剂
初步U. S.批准：2011

适应症
TRADJENTA是一个二肽基肽酶-4（DPP - 4）抑制剂作为辅助饮食和运动改善血糖控制与2型糖尿病成人表示

使用重要的限制：

不应该用在1型糖尿病患者或糖尿病酮症酸中毒的治疗尚未研究相结合，与胰岛素

剂量和用法
TRADJENTA建议剂量为5毫克，每日一次。 TRADJENTA可以采取带或不带食品。
 
剂型和优势
片剂：5毫克

禁忌
过敏反应，如荨麻疹，血管神经性水肿或支气管的高反应性以linagliptin的历史，

警告和注意事项
胰岛素secretagogue（如磺脲类）使用时，考虑降低胰岛素secretagogue的剂量，以减少低血糖的风险有没有建立大血管病变与TRADJENTA风险减少或任何其他降糖药物的确凿证据临床研究

不良反应
在≥5％TRADJENTA和更普遍比安慰剂治疗的患者治疗的患者报告的不良反应包括鼻咽炎低血糖症是较为常用TRADJENTA和磺脲类治疗的患者相比，那些组合与安慰剂组和磺脲类治疗
胰腺炎往往在患者linagliptin（1每538人年，与零比较器在433人年）
 
药物相互作用
P-glycoprotein/CYP 3A4诱导剂：结合时（如利福平）TRADJENTA疗效可能会减少。强烈建议使用替代疗法。
 
在特殊人群中使用
怀孕：孕妇有没有足够和良好对照的研究。 TRADJENTA片应在怀孕期间使用，只有在明确需要。
哺乳母亲：应谨慎时TRADJENTA管理到哺乳期妇女
儿科患者：18岁以下的患者的安全性和有效性TRADJENTA尚未确定 肾或肝功能不全：无剂量调整的建议。

修订日期：05/2011

Tradjenta is expected to be available in May 2011 in a 5mg dosage strength.

利拉利汀（Tradjenta）在治疗2型糖尿病时，可以单独使用，也可以联合使用。目前在美国上市，剂型，片剂。

linagliptin（利拉利汀）:糖尿病的上市新药
美国食品和药物管理局2011年5月2日批准一种治疗Ⅱ型糖尿病的口服药片Tradjenta(linagliptin tablets，通用名“利拉利汀”，结构式见下图）上市，利拉利汀可用于改善Ⅱ型糖尿病患者血糖控制能力。在约3800名Ⅱ型糖尿病患者参与的8项双盲临床试验中，Tradjenta的安全性和有效性得到展现，其主要副作用包括上呼吸道感染、流鼻涕、喉咙痛、肌肉痛和头痛等。

Ⅱ型糖尿病又称成年发病型糖尿病，是最常见的糖尿病，其特点是胰岛素抵抗，即自体能够产生胰岛素，但体内组织对胰岛素的作用不敏感，正常量的胰岛素起不到正常的降血糖作用。利拉利汀通过抑制二肽基肽酶－4，提高一种激素的水平，而这种激素可刺激胰岛素释放，进而改善服用者的血糖控制。利拉利汀由位于美国康涅狄格州的勃林格殷格翰制药公司出品，可单独服用，也可与其他现有药物联合使用。

Tradjenta
Generic Name: linagliptin
Date of Approval: May 2, 2011
Company: Boehringer Ingelheim Pharmaceuticals, Inc. and Eli Lilly and Company

Linagliptin (Tradjenta) Possible Approval for Use in Europe for Type 2 Treatment: Linagliptin (sold under the name Tradjenta) has been available in the United States for those with type 2 diabetes since May 2011, when the Food and Drug Administration gave their approval for its use at that time. Tradjenta is an oral medication and comes in 5 mg tablets.

Tradjenta has proven to be effective for those with type 2 diabetes who had difficulties tolerating metformin or those with kidney problems. Tradjenta is used along with diet and exercise to lower blood sugar levels.

Tradjenta is not approved for use in conjunction with insulin or for the use in children. Tradjenta can cause low blood sugar levels, resulting in insulin reactions.

In June 2011, Boehringer Ingelheim and Eli Lilly and Company, the makers of linagliptin, received a positive response from the European Medicines Agency’s (EMA) Medicinal Committee recommending that linagliptin in the 5 mg dose, film-coated tablets, be approved for use in Europe. “The Committee for Medicinal Products for Human Use (CHMP) has recommended the approval of linagliptin as a monotherapy in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to intolerance, or contraindicated due to renal impairment.” They are also recommending that linagliptin might be used in combination with metformin and metformin plus sulfonylurea. Their research showed that when linagliptin was used in conjunction with metformin, it reduced the A1C levels by 0.6 to 0.7 percent when compared to the use of a placebo. The positive opinion for the use in Europe of linagliptin was based on a clinical trial program that involved approximately 4,000 adults with type 2 diabetes.

Professor Anthony Barnett, Clinical Director, Department of Diabetes and Endocrinology, University of Birmingham and Heart of England NHS, UK, was quoted as saying, “This will be an important step forward in the management of type 2 diabetes in Europe.” Furthermore, he stated, “Of note, linagliptin is primarily excreted via the bile and gut, meaning no dose adjustment is recommended in patients with kidney or liver impairment. Therefore, this will be the first DPP-4 inhibitor available at one dose for all adult patients with type 2 diabetes.”

Type 2 diabetes has increasingly been diagnosed around the world. Linagliptin will be a new treatment available in the UK for those suffering from type 2 diabetes and are having difficulties controlling their blood sugar levels.

Boehringer Ingelheim and Eli Lilly and Company are part of a worldwide alliance that was formed in January 2011. Enrique Conterno, President of Lilly Diabetes was quoted as saying, “We are extremely pleased by the CHMP positive recommendation for approval of linagliptin in Europe. Based on our comprehensive studies and the CHMP’s positive recommendation, we believe linagliptin can be an important new treatment option for adult patients with type 2 diabetes.”