注射用TANZEUM (阿必鲁泰[albiglutide])为成为第三个获得美国FDA批准上市的GLP-1受体激动剂
美国初次批准：2014
适应证和用途
TANZEUM是一种GLP-1受体激动剂适用为一种对饮食和锻炼辅助在有2型糖尿病成年中改善血糖控制。
使用的限制：
⑴对饮食和锻炼控制不佳患者不建议作为一线治疗。
⑵尚未在有胰腺炎患者中研究。在有胰腺炎史患者考虑其他糖尿病治疗方法。
⑶不为1型糖尿病或糖尿病酮症酸中毒治疗。
⑷不为患者有预先存在严重胃肠道疾病。
⑸尚未研究与餐前胰岛素联用。
剂量和给药方法
⑴在一天中的任何时间每周给药1次，与进食无关.
⑵在腹部，大腿或上臂皮下注射。
⑶开始30mg皮下每周1次。在需要附加血糖控制患者剂量可增至50mg每周1次。
⑷如丢失一剂，丢失剂量3天内给予丢失剂量。 见完整处方资料和为冻干粉重建和给药使用患者指导。
剂型和规格
注射用：在一支单剂量笔30mg或50mg。
禁忌证
⑴甲状腺髓样癌的个人或家族史或在有多发性内分泌腺瘤综合征2型患者。
⑵对阿必鲁泰或任何产品组分严重超敏性史。
警告和注意事项
⑴胰腺炎：如怀疑及时终止。如确证不要再开始。有胰腺炎史患者考虑其他糖尿病治疗方法。
⑵低血糖：当与胰岛素促泌剂联用时可能发生(如，磺脲类[sulfonylureas])或胰岛素。当开始TANZEUM时考虑降低磺脲类或胰岛素剂量。
⑶超敏性反应：如怀疑终止TANZEUM。监视和标准护理及时治疗直至体征和症状解决。
⑷肾受损：有肾受损患者监视肾功能报告严重不良胃肠道反应。
⑸大血管结局：尚无临床试验确定用TANZEUM或任何其他抗糖尿病药物减低大血管风险的结论性证据。
不良反应
不良反应，用TANZEUM治疗患者报告 ≥10%和比用安慰剂患者更频，为上呼吸道感染，腹泻，恶心，和注射部位反应。
药物相互作用
TANZEUM延迟胃排空。可能影响同时给予口服药物的吸收。
特殊人群中使用
⑴妊娠：TANZEUM可能致胎儿危害；只有如潜在获益胜过对胚胎潜在风险才使用。
⑵哺乳母亲：终止哺乳或终止TANZEUM。
⑶肾受损：建议不调整剂量。有肾受损患者监视肾功能报道严重不良胃肠道反应。

GSK receives US approval for once-weekly type 2 diabetes treatment, Tanzeum™ (albiglutide)
LONDON, April 15, 2014 /PRNewswire/ -- GlaxoSmithKline plc (LSE/NYSE: GSK) today announced that the US Food and Drug Administration (FDA) has approved Tanzeum™ (albiglutide) for injection, for subcutaneous use, as a once-weekly treatment for type 2 diabetes. Tanzeum has been approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Albiglutide, a glucagon-like peptide-1 receptor agonist (GLP-1), is a biological product for the treatment of type 2 diabetes, administered once-weekly using an injector pen supplied with a 5mm 29-gauge thin-walled needle. Glucagon-like peptide-1 is an important incretin hormone that helps reduce blood glucose levels but, in people with type 2 diabetes, its production is often reduced or absent.
Vlad Hogenhuis, Senior Vice-President and Head, GSK Global Cardiovascular, Metabolic and Neurosciences Franchise, said: "Many type 2 diabetes patients struggle to keep their blood sugar within the recommended levels. We are pleased that the approval of Tanzeum provides an effective new weekly GLP-1 treatment option for appropriate patients in the US."
The FDA approval of albiglutide is based on the results of GSK's comprehensive Phase III Harmony programme, consisting of eight trials and involving over 5,000 patients, over 2,000 of whom were treated with Tanzeum. The Harmony studies evaluated albiglutide against commonly-used classes of type 2 diabetes treatment, including insulin, metformin, glimepiride and pioglitazone, in patients at different stages of the disease, as well as those with renal impairment.
Following this approval by the FDA, GSK anticipates the US launch of Tanzeum in the third quarter of 2014.
Albiglutide was licensed by the European Medicines Agency in March 2014, under the brand name Eperzan®, for use in adult patients with type 2 diabetes.
About diabetes
Diabetes is a global epidemic, affecting 382 million individuals globally, over 20 million of whom are in the US.1 Up to 95% of these patients have type 2 diabetes.1 Type 2 diabetes is a life-long, progressive and, in some cases, preventable condition characterized by high blood sugar levels, known as hyperglycemia.  A lack of physical activity, obesity, increasing age, high blood pressure and genetics are known risk factors that can contribute to the development of type 2 diabetes.2,3  Treatment options include lifestyle changes such as increased physical activity and diet but, as the condition progresses, patients may require the addition of oral and injectable medications to control blood sugar levels and, ultimately, the use of insulin, either daily or with meals.
About Tanzeum™ (albiglutide)
Tanzeum is a GLP-1 receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
LIMITATIONS OF USE
Tanzeum is not recommended as first-line therapy for patients inadequately controlled on diet and exercise. Tanzeum has not been studied in patients with a history of pancreatitis. Tanzeum is not for treatment of type 1 diabetes mellitus or diabetic ketoacidosis. Tanzeum has not been studied in patients with pre-existing severe gastrointestinal disease. Tanzeum has not been studied in combination with prandial insulin.
Full US Prescribing Information, including BOXED WARNING, Medication Guide and Instructions for Use will soon be available at us.gsk.com.  Prior to the label being posted online, a copy of the label may be requested from the GSK Media or Investor Relations contacts listed in the "GlaxoSmithKline Inquiries" section at the end of this document.
Tanzeum has been approved with a Risk Evaluation and Mitigation Strategy (REMS), required by the FDA to ensure that the benefits of Tanzeum outweigh the potential risk of medullary thyroid carcinoma and the risk of acute pancreatitis.  A non-promotional factsheet, reviewed by the FDA, with more detailed safety information is available at www.TANZEUMREMS.com.
Important Safety information for Tanzeum (albiglutide)
The following information is taken from the highlights section of the US Prescribing Information.  Please see full Prescribing Information including boxed warning.
BOXED WARNING: RISK OF THYROID C-CELL TUMORS
Thyroid C-cell tumors have been observed in rodent studies with glucagon-like peptide-1 (GLP-1) receptor agonists at clinically relevant exposures. It is unknown whether Tanzeum causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans. Tanzeum is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2).
CONTRAINDICATIONS
Do not use in patients with a personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). Do not use in patients with a prior serious hypersensitivity reaction to albiglutide or to any of the product components.
WARNINGS AND PRECAUTIONS
Pancreatitis: Discontinue promptly if suspected. Do not restart if confirmed. Consider other antidiabetic therapies in patients with a history of pancreatitis.
Hypoglycemia: Can occur when used in combination with insulin secretagogues (e.g. sulfonylureas) or insulin. Consider lowering sulfonylurea or insulin dosage when starting Tanzeum.
Hypersensitivity Reactions: Discontinue Tanzeum if suspected. Monitor and treat promptly per standard of care until signs and symptoms resolve.
Renal Impairment: Monitor renal function in patients with renal impairment reporting severe adverse gastrointestinal reactions.
Macrovascular Outcomes: There have been no clinical trials establishing conclusive evidence of macrovascular risk reduction with Tanzeum or any other antidiabetic drug.
ADVERSE REACTIONS
Adverse reactions, reported in >/=10% of patients treated with Tanzeum and more frequently than in patients on placebo, were upper respiratory tract infection, diarrhea, nausea, and injection site reaction.
FDA批准一周一次GLP-1类新药阿必鲁肽上市
美国FDA于当地时间4月15日批准葛兰素史克新药阿必鲁肽（Albiglutide；商品名Tanzeum）结合饮食与运动用于改善2型糖尿病成人患者的血糖控制。
阿必鲁肽是一种长效的胰高血糖素样肽-1（GLP-1）受体激动剂，为皮下注射剂，每周注射一次。“对美国约2400万2型糖尿病患者来说，阿必鲁泰是一种新的治疗选择。阿必鲁泰可以单独使用，或在现有治疗方案基础上联用以控制血糖水平”，FDA药品评价与研究中心药物评价II办公室主任Curtis Rosebraugh博士称。
阿必鲁肽的安全性及有效性已在8项由2000多名2型糖尿病患者参与的临床试验中得到评价，它能有效改善参与试验患者的HbA1c水平。阿必鲁肽可以和与其它2型糖尿病药物（包括二甲双胍、格列美脲、吡格列酮及胰岛素）联合用药。
阿必鲁肽不适用于治疗1型糖尿病患者，以及血液及尿液酮体水平升高(即糖尿病酮症酸中毒)的患者，也不能作为饮食和运动无法有效控制血糖的糖尿病患者的一线治疗药物.
阿必鲁肽带有一项黑框警告（曾在某些使用GLP-1受体激动剂的啮齿类动物研究中发现有甲状腺肿瘤风险），但目前尚未确定阿必鲁肽是否会导致甲状腺C细胞瘤或甲状腺髓样瘤（MTC）。因此，阿必鲁泰不应用于个人或家庭有MTC病史的患者，也不能用于2型多发性内分泌腺瘤综合征患者（此类患者有MTC发病倾向）。
FDA要求对阿必鲁肽进行三项上市后研究：一项在儿科患者身上评价给药剂量、有效性及安全性的临床试验；一项至少15年期的甲状腺髓样瘤登记研究，以确定甲状腺髓样瘤的发生率是否与阿必鲁泰有关联;一项心血管结局试验（CVOT），评价阿必鲁泰在心血管疾病高基线风险患者身上的心血管风险。
在临床研究中，阿必鲁肽用药患者最常出现的不良反应是腹泻、恶心和注射部位反应。FDA要求阿必鲁肽实施一项风险评估和减轻战略（REMS），随时告知卫生保健提供商阿必鲁肽相关的严重风险。
据悉，阿必鲁肽是FDA批准的第二个长效GLP-1类似物（FDA之前还批准了缓释艾塞那肽Bydureon），该药已在3月26日获得欧洲药品管理局人用医药产品委员会（EMA）批准上市（商品名Eperzan）。