勃林格-礼来在美国推出糖尿病复方新药Glyxambi

勃林格-礼来糖尿病联盟近日联合在美国推出糖尿病复方新药Glyxambi，该药是首个双效抑制剂降糖药，由已上市药物Jardiance（empagliflozin，一种钠-葡萄糖联合转运体-2（SGLT2）抑制剂）和Trajenta（linagliptin，一种二肽基肽酶-4抑制剂（DPP-4））组成。FDA于今年2月批准Glyxambi作为每日一次的口服药物，辅助饮食和运动用于改善2型糖尿病成人患者的血糖控制。Glyxambi是一种每日一次的片剂，在每天早上服药，该药由10mg或25mg SGLT2抑制剂empagliflozin和5mgDPP-IV抑制剂linagliptin组成。Glyxambi不适用于1型糖尿病或糖尿病酮症酸中毒的治疗。

empagliflozin属于钠-葡萄糖协同转运蛋白-2（SGLT-2）抑制剂类药物，开发用于2型糖尿病成人患者的治疗。新兴的SGLT-2抑制剂类药物，已被证实能够阻断肾脏中葡萄糖的再吸收作用，将过多的葡萄糖通过尿液排泄到体外，从而达到降低血糖水平的效果，而且该降糖效果不依赖于β细胞功能和胰岛素抵抗。

linagliptin则属于二肽基肽酶-4（DPP-4）抑制剂类药物，可刺激刺激胰腺分泌更多的胰岛素，并刺激肝脏产生更少的葡萄糖。目前，linagliptin已在美国上市，品牌名为Tradjenta，作为每日一次的药物，结合饮食和运动改善2型糖尿病成人患者的血糖控制。

Glyxambi是首个将这2种具独特作用机制的药物合并至单一片剂的复方新药，该药也是勃林格-礼来糖尿病联盟联合开发的重要产品之一。

英文原文：First-in-class type 2 diabetes treatment Glyxambi? (empagliflozin/linagliptin) tablets for adults now available in U.S. pharmacies

New dual inhibitor SGLT2/DPP-4 combination therapy offers improved glycemic control as an adjunct to diet and exercise

New GLYXAMBI savings program offered for eligible patients

RIDGEFIELD, Conn., and INDIANAPOLIS, March 23, 2015 /PRNewswire/ -- Glyxambi? (empagliflozin/linagliptin) tablets are now available by prescription in many leading chain and independent pharmacies across the U.S., including Walgreens and Rite Aid. GLYXAMBI, part of the Boehringer Ingelheim Pharmaceuticals, Inc. (BIPI) and Eli Lilly and Company (LLY) Diabetes alliance portfolio, is the first and only dual inhibitor combination therapy approved in the U.S. to combine the mechanisms of action of a sodium glucose co-transporter-2 (SGLT2) inhibitor and a dipeptidyl peptidase-4 (DPP-4) inhibitor in a once-daily tablet.

GLYXAMBI is approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes (T2D) when both empagliflozin and linagliptin are appropriate treatments. GLYXAMBI is a once-daily tablet taken in the morning that combines 10 mg or 25 mg of empagliflozin, an SGLT2 inhibitor, with 5 mg of linagliptin, a DPP-4 inhibitor. GLYXAMBI is not for people with type 1 diabetes or for diabetic ketoacidosis (increased ketones in the blood or urine). If you have had pancreatitis (inflammation of the pancreas) it is not known if you have a higher chance of getting pancreatitis while taking GLYXAMBI.

"The rapid market availability of GLYXAMBI following its recent FDA approval in late January is a reflection of Boehringer Ingelheim and Lilly's commitment to bringing new treatment options to people with type 2 diabetes," said Kathleen Dowd, senior vice president, marketing, Boehringer Ingelheim Pharmaceuticals, Inc. "As the fourth diabetes medicine to emerge from our alliance pipeline in the U.S., we believe GLYXAMBI may help adults with type 2 diabetes lower their blood sugar and manage their diabetes."

A GLYXAMBI savings card program is available online and in many doctors' offices for patients who qualify. For terms and conditions and any questions regarding eligibility or benefits, visit GLYXAMBIsavings.com or call 1-855-GLYXAMBI (1-855-459-9262).

GLYXAMBI should not be taken if you have severe kidney problems, are on dialysis or if you are allergic to empagliflozin and linagliptin or any of the ingredients in GLYXAMBI. Symptoms of a serious allergic reaction to GLYXAMBI may include skin rash, itching, flaking or peeling; raised red patches on your skin (hives); difficulty swallowing or breathing; or swelling of your face, lips, tongue, and throat that may cause difficulty breathing or swallowing. If you have any of these symptoms, stop taking GLYXAMBI and call your doctor or go to the emergency room right away.

"As an add-on to metformin, GLYXAMBI was superior in reducing A1C when compared with either empagliflozin or linagliptin alone," said David Kendall, M.D., vice president, medical affairs, Lilly Diabetes. "The management of type 2 diabetes requires a personalized treatment plan, and GLYXAMBI provides patients and their physicians with a new option to help improve blood sugar control."

The U.S. Food and Drug Administration approval was based on a phase III clinical trial that evaluated the efficacy and safety of GLYXAMBI (10/5 mg and 25/5 mg) compared with the individual components of empagliflozin (10 mg or 25 mg) or linagliptin (5 mg) in adults with T2D who were also taking high-dose metformin (mean dose 1889 mg daily). The study, which randomized 686 adults with T2D and hemoglobin A1C (a measure of average blood glucose over the past two to three months) between 7.0 and 10.5 percent, examined the change from baseline in A1C at 24 weeks. The study demonstrated superior A1C reduction with GLYXAMBI compared with the individual components of empagliflozin or linagliptin. Starting from a mean baseline of approximately 8.0 percent, adults in this trial achieved a mean A1C of 6.9 and 6.7 percent with GLYXAMBI 10/5 mg and 25/5 mg, respectively, compared with a mean A1C of 7.3 and 7.4 percent for empagliflozin 10 mg and 25 mg, respectively, and 7.3 percent for linagliptin 5 mg.

Data recently published in Diabetes Care demonstrated that 58 percent and 62 percent of patients taking GLYXAMBI 10/5 mg or 25/5 mg, respectively, in addition to metformin achieved an A1C of less than 7 percent from a baseline A1C of approximately 8 percent, compared with 28 percent of patients taking empagliflozin 10 mg, 33 percent taking empagliflozin 25 mg and 36 percent taking linagliptin 5 mg.

Through 52 weeks, the safety profile of GLYXAMBI was demonstrated in a pooled analysis, and the most common adverse reactions were urinary tract infection (UTI) (12.5 percent and 11.4 percent for GLYXAMBI 10/5 mg and 25/5 mg, respectively; through 52 weeks, no patient discontinued GLYXAMBI due to UTIs), nasopharyngitis (5.9 percent and 6.6 percent for GLYXAMBI 10/5 mg and 25/5 mg, respectively) and upper respiratory tract infection (7.0 percent for GLYXAMBI 10/5 mg and 25/5 mg).

Serious side effects can happen to people taking GLYXAMBI, including inflammation of the pancreas (pancreatitis), which may be severe and lead to death. Before you start taking GLYXAMBI, tell your doctor if you have ever had pancreatitis, gallstones, a history of alcoholism, or high triglyceride levels. Stop taking GLYXAMBI and call your doctor right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may be felt going from your abdomen to your back. The pain may happen with or without vomiting. These may be symptoms of pancreatitis.

What is GLYXAMBI?
GLYXAMBI is a prescription medicine that contains 2 diabetes medicines, empagliflozin and linagliptin.  GLYXAMBI can be used along with diet and exercise to lower blood sugar in adults with type 2 diabetes when treatment with both empagliflozin and linagliptin is appropriate.