英文药名：TANZEUM(albiglutide)injection 中文药名：阿必鲁泰注射剂 生产厂家：葛兰素史克（GSK） 药品介绍 近日，美国推出糖尿病新药Tanzeum（albiglutide），该药为每周一次的皮下注射药物，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。 注射用TANZEUM (阿必鲁泰[albiglutide])为皮下使用 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30 mg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。 Indications and Usage for TANZEUM TANZEUM is an injectable prescription medicine that may improve blood sugar (glucose) in adults with type 2 diabetes, and should be used along with diet and exercise. TANZEUM is not recommended as the first medication to treat diabetes. TANZEUM has not been studied in people who previously had pancreatitis. TANZEUM is not a substitute for insulin and is not for people with type 1 diabetes or diabetic ketoacidosis. TANZEUM is not recommended in people with severe stomach or intestinal problems. It is not known if TANZEUM can be used with short-acting or rapid-acting (mealtime) insulin. TANZEUM has not been studied in children under 18 years of age. IMPORTANT SAFETY INFORMATION In studies with rats and mice, medicines that work like TANZEUM caused thyroid tumors, including thyroid cancer. It is not known if TANZEUM will cause thyroid tumors or a type of thyroid cancer called medullary thyroid carcinoma (MTC) in people. Do not use TANZEUM if you or your family have ever had MTC or if you have an endocrine system cancer called Multiple Endocrine Neoplasia syndrome type 2. Tell your healthcare provider if you get a lump or swelling in your neck, hoarseness, trouble swallowing, or shortness of breath. These may be symptoms of thyroid cancer. Do not use TANZEUM if you are allergic to albiglutide or any of the ingredients in TANZEUM. Before using TANZEUM, tell your healthcare provider about your medical conditions, including if you have or have had problems with your pancreas, kidneys, or liver, have severe problems with your stomach, such as slowed emptying of your stomach (gastroparesis) or problems with digesting food. Tell your healthcare provider if you are taking a new prescription or over-the-counter medicines, vitamins, or herbal supplements. Tell your healthcare provider if you are pregnant or plan to become pregnant. It is not known if TANZEUM will harm your unborn baby. Tell your healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if TANZEUM passes into your breast milk. TANZEUM may cause serious side effects, including: •inflammation of your pancreas (pancreatitis). Stop using TANZEUM and call your healthcare provider right away if you have severe pain in your stomach area (abdomen) that will not go away, with or without vomiting. You may feel pain that may go from your abdomen to your back. •low blood sugar (hypoglycemia). Your risk is higher if you take TANZEUM with another medicine that can cause low blood sugar such as insulin or a sulfonylurea. Signs and symptoms of low blood sugar may include dizziness or light-headedness, sweating, confusion, headache, blurred vision, slurred speech, shakiness, fast heart beat, anxiety, irritability, or mood changes, hunger, and feeling jittery. •allergic reactions. Stop using TANZEUM and get medical help right away if you have any symptoms of an allergic reaction, including itching, rash, or difficulty breathing. •kidney problems (kidney failure). In people who have kidney problems, diarrhea, nausea, and vomiting may result in loss of fluids (dehydration), which may worsen kidney problems. Common side effects of TANZEUM may include diarrhea, nausea, reactions at your injection site, cough, back pain, and cold or flu symptoms. These are not all the possible side effects of TANZEUM. For more information, talk to your healthcare provider. TANZEUM Rx Pharmacological Class: Glucagon-like peptide-1 (GLP-1) receptor agonist. Active Ingredient(s): Albiglutide [recombinant fusion protein] 30mg, 50mg; per Pen; lyophilized pwd for SC inj after reconstitution; preservative-free. Company GlaxoSmithKline Pharmaceuticals Indication(s): Adjunct to diet and exercise, to improve glycemic control in adults with type 2 diabetes. Limitations of use: not recommended as first-line treatment for patients inadequately controlled on diet and exercise. Not studied in combination with prandial insulin or with history of pancreatitis. Not for treating type 1 diabetes or diabetic ketoacidosis. Not a substitute for insulin. Not recommended in patients with pre-existing severe GI disease. Pharmacology: Tanzeum is an agonist of the GLP-1 receptor and augments glucose-dependent insulin secretion. GLP-1 also suppresses glucagon secretion during periods of hyperglycemia and slows gastric emptying. Clinical Trials: Tanzeum was studied as monotherapy and in combination with metformin, metformin + sulfonylurea, thiazolidinedione ± metformin, and insulin glargine ± oral antidiabetics. The efficacy of Tanzeum was compared with placebo, glimepiride, pioglitazone, liraglutide, sitagliptin, insulin lispro, and insulin glargine. Tanzeum as monotherapy was evaluated in a 52-week, randomized, double-blind, placebo-controlled, multicenter trial in patients with type 2 diabetes (n=296). Patients were randomized to Tanzeum 30mg SC once weekly, Tanzeum 30mg SC once weekly uptitrated to 50mg once weekly at Week 12, or placebo. The primary endpoint was the mean change in HbA1c from baseline to Week 52. Results showed that Tanzeum 30mg had a mean change in HbA1c of −0.7% (difference from placebo −0.8; [95% CI: −1.1, −0.6]) and Tanzeum 50mg had a mean change in HbA1c of −0.9% (difference from placebo −1.0; [95% CI: −1.3, −0.8]). Compared with placebo, treatment with Tanzeum 30mg and 50mg resulted in statistically significant reductions in HbA1c from baseline at Week 52 (P<0.0001). The efficacy of Tanzeum was also evaluated as combination therapy in a 104-week randomized, double-blind, multicenter trial in patients with type 2 diabetes (n=999) inadequately controlled on background metformin therapy (≥1,500mg daily). Patients were randomized to Tanzeum 30mg once weekly with optional uptitration to 50mg after minimum of 4 weeks (n=297), placebo (n=100), sitagliptin 100mg daily (n=300), or glimepiride 2mg daily (n=302). Results in this trial showed the change in HbA1c for Tanzeum was −0.6% (difference from placebo −0.9; [95% CI: −1.16, −0.65], sitagliptin −0.4; [95% CI: −0.53, −0.17], and glimepiride −0.3; [95% CI: −0.45, −0.09]). Compared with placebo, sitagliptin, and glimepiride, treatment with Tanzeum resulted in significantly greater reduction in HbA1c from baseline at Week 104 (P<0.0137). For more clinical trial data, see full labeling. Legal Classification: Rx Adults: Give by SC inj in the abdomen, thigh, or upper arm on the same day each week without regard to meals. Initiate at 30mg once weekly; may increase to 50mg once weekly if inadequate response. Renal impairment: caution with initiating or escalating doses. Children: <18years: not established. Contraindication(s): History (personal or family) of medullary thyroid carcinoma. Multiple endocrine neoplasia syndrome type 2. Warnings/Precautions: Inform patients of thyroid cancer risk and symptoms. Monitor for pancreatitis; discontinue if suspected; do not restart if confirmed. History of pancreatitis; consider other antidiabetic therapies. Discontinue if hypersensitivity occurs. Monitor renal function in renally-impaired patients reporting severe GI reactions. Pregnancy (Category C). Nursing mothers: not recommended. Interaction(s) Increased risk of hypoglycemia with concomitant sulfonylureas or insulin; consider reducing their doses. May affect absorption of other oral drugs (delayed gastric emptying). Adverse Reaction(s) Upper respiratory tract infection, diarrhea, nausea, injection site reaction; acute pancreatitis. How Supplied: Single-dose Pen—4 LAST UPDATED: 8/29/2014 美国FDA批准一周一次GLP-1类新药阿必鲁肽上市 2014年4月16日，美国FDA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）。