2016年5月31日勃林格殷格翰-礼来糖尿病联盟近日宣布，FDA已批准糖尿病复方新药Jentadueto XR（利拉利汀/盐酸二甲双胍缓释）片剂，用于2型糖尿病（T2D）成人患者的治疗。Jentadueto XR由勃林格殷格翰（BI）和礼来联合销售，该药是勃林格-礼来糖尿病联盟在过去5年中获得FDA批准的第7个糖尿病新药。
Jentadueto XR是由2.5mg或5mg的linagliptin（利拉利汀）和1000mg的二甲双胍组成的复方药。利拉利汀是一种二肽基肽酶-4（DPP-4）抑制剂，而二甲双胍常处方用于2型糖尿病的早期治疗。
Jentadueto XR适用于结合饮食和运动，用于适合利拉利汀和二甲双胍治疗的2型糖尿病患者，以改善血糖控制。Jentadueto XR不适用于1型糖尿病和糖尿病酮症酸中毒的治疗，该药在伴有胰腺炎病史的群体中尚未开展研究。
需要指出的是，Jentadueto XR的处方标签中含有一个带框警告，提示该药的乳酸性酸中毒风险，这是一种严重的代谢并发症，在Jentadueto XR治疗期间因二甲双胍积累时可能会发生。
利拉利汀是一种高效的二肽基肽酶-4（DPP-4）抑制剂，通过选择性抑制DPP-4，可以升高内源性胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性促胰岛素释放多肽（GIP）的水平，从而调节血糖。进餐后GLP-1在肠道即时分泌，进而刺激胰腺产生葡萄糖依赖性胰岛素分泌，同时抑制胰高血糖素分泌，延迟胃排空。在生理状态下，DPP-4可快速降解GLP-1和GIP，使其失去活性，而服用DPP-4抑制剂可以使内源性GLP-1水平升高3-4倍，有效降低HbA1c和餐后血糖，且不影响体重，同时没有明显的低血糖风险。
附完整处方资料：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3d02a4d4-d312-80b4-05c4-691b8f0aa7aa
Boehringer Ingelheim and Lilly's (LLY) Jentadueto XR Approved by U.S. FDA
The U.S. Food and Drug Administration (FDA) has approved Jentadueto XR (linagliptin and metformin hydrochloride extended-release) tablets for the treatment of type 2 diabetes (T2D) in adults. JENTADUETO XR, which is marketed by Boehringer Ingelheim and Eli Lilly and Company (NYSE: LLY), is the seventh new treatment from the Boehringer Ingelheim-Lilly Diabetes alliance to be approved by the FDA in the last five years.
JENTADUETO XR combines 2.5 mg or 5 mg of linagliptin with 1000 mg of metformin. Linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, works by increasing hormones that stimulate the pancreas to produce more insulin and the liver to produce less glucose. Metformin, a commonly prescribed initial treatment for T2D, lowers glucose production by the liver and its absorption in the intestine.
"Adults with type 2 diabetes are often required to take more than one medication to manage their condition, including some that have to be taken multiple times a day," said Paul Fonteyne, president and CEO, Boehringer Ingelheim Pharmaceuticals, Inc. "JENTADUETO XR, the first extended-release therapy to emerge from our alliance with Lilly, offers adults with type 2 diabetes the convenience of a combination pill taken once a day to help lower blood sugar levels."
JENTADUETO XR is indicated as an adjunct to diet and exercise to improve glycemic control in adults with T2D when treatment with both linagliptin and metformin is appropriate. JENTADUETO XR should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis, and has not been studied in people with a history of pancreatitis.
The JENTADUETO XR label contains a boxed warning for the risk of lactic acidosis, a serious metabolic complication that can occur due to metformin accumulation during treatment with JENTADUETO XR.
The safety and efficacy of JENTADUETO XR have been established based on adequate and well-controlled studies of linagliptin and metformin co-administered in patients with T2D inadequately controlled on diet and exercise and in combination with sulfonylurea. |
