2015年3月23日訊 /生物谷BIOON/ --勃林格-禮來糖尿病聯盟近日聯合在美國推出糖尿病複方新藥Glyxambi，該藥是首個雙效抑制劑降糖藥，由已上市藥物Jardiance（empagliflozin，一種鈉-葡萄糖聯合轉運體-2（SGLT2）抑制劑）和Trajenta（linagliptin，一種二肽基肽酶-4抑制劑（DPP-4））組成。FDA於今年2月批准Glyxambi作為每日一次的口服藥物，輔助飲食和運動用於改善2型糖尿病成人患者的血糖控制。Glyxambi是一種每日一次的片劑，在每天早上服藥，該藥由10mg或25mg SGLT2抑制劑empagliflozin和5mgDPP-IV抑制劑linagliptin組成。Glyxambi不適用於1型糖尿病或糖尿病酮症酸中毒的治療。
empagliflozin屬於鈉-葡萄糖協同轉運蛋白-2（SGLT-2）抑制劑類藥物，開發用於2型糖尿病成人患者的治療。新興的SGLT-2抑制劑類藥物，已被證實能夠阻斷腎臟中葡萄糖的再吸收作用，將過多的葡萄糖通過尿液排洩到體外，從而達到降低血糖水平的效果，而且該降糖效果不依賴於β細胞功能和胰島素抵抗。
linagliptin則屬於二肽基肽酶-4（DPP-4）抑制劑類藥物，可刺激刺激胰腺分泌更多的胰島素，並刺激肝臟產生更少的葡萄糖。目前，linagliptin已在美國上市，品牌名為Tradjenta，作為每日一次的藥物，結合飲食和運動改善2型糖尿病成人患者的血糖控制。
Glyxambi是首個將這2種具獨特作用機制的藥物合併至單一片劑的複方新藥，該藥也是勃林格-禮來糖尿病聯盟聯合開發的重要產品之一。（生物谷Bioon.com）
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.