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商品名：Onglyza 通用名：Saxagliptin沙格列汀 Saxagliptin为白色到淡黄色或者淡棕色，非吸湿性，结晶性粉末。在24°C ± 3°C水中难溶，乙酸乙酯微溶，溶于甲醇，乙醇，异丙醇，乙腈，丙酮，聚乙二醇400（聚乙二醇400）。 Saxagliptin是二肽基肽酶抑制剂类抗糖尿病治疗药物之一，为近几年关注度极高的新型II型糖尿病治疗药物。其主要是通过抑制体内的二肽酰肽酶IV（dipeptidyl peptidase IV，DDP-IV），以减少血液中胰高血糖素样多肽（GLP-1）的分解和代谢，提高血液中胰高血糖素样多肽的浓度达到提高胰岛素水平，发挥降糖作用。 ONGLYZA（saxagliptin）片 美国首次批准：2009 使用的重要限制： 不应该用于治疗1型糖尿病或糖尿病酮症酸中毒。
重要的安全性信息 与已知会引起低血糖的药物合用：胰岛素促泌剂，如磺脲类，会引起低血糖。因此，与ONGLYZA™合用时，需减少胰岛素促泌剂的剂量，以降低发生低血糖的风险。 大血管风险终点事件研究：目前尚无此类结论性的临床研究证明ONGLYZA™ (saxagliptin)或其他任何糖尿病治疗药物可降低大血管并发症的风险。 最常见的不良反应（无论研究者对因果关系的评估如何）：ONGLYZA™治疗的患者中，发生率≥5%且高于对照组患者发生率的不良反应为上呼吸道感染（7.7%，7.6%）、头痛（7.5%，5.2%）、鼻咽炎（6.9%，4.0%）和尿路感染（6.8%，6.1%）。噻唑烷二酮类联用治疗时，ONGLYZA™2.5mg、5mg和安慰剂的外周性水肿发生率分别为3.1%、8.1%和4.3%。 药物相互作用：由于CYP 3A4/5强抑制剂酮康唑可增加沙格列汀（saxagliptin）暴露量，当ONGLYZA™与CYP 3A4/5强抑制剂（如阿扎那韦、克拉霉素、茚地那韦、伊曲康唑、酮康唑、奈法唑酮、奈非那韦、利托那韦、沙奎那韦和泰利霉素）合用时，应限制剂量为2.5mg。 肾功能不全患者：为中度或重度肾功能不全患者或需要血液透析的终末期肾病（肌酐清除率≤50mL/min）患者每日给予ONGLYZA™2.5mg 1次，应在血液透析后给药。目前尚未在接受腹膜透析治疗的患者中对ONGLYZA™进行研究。开始ONGLYZA™治疗前及治疗开始后应定期评估肾功能。 孕妇及哺乳期妇女：没有在孕妇中开展充分且良好对照的研究。与其它糖尿病治疗药物一样，ONGLYZA™只有在明显需要时才能用于孕妇。目前尚不清楚沙格列汀（saxagliptin）是否会通过人类母乳分泌。由于很多药物都通过人类母乳分泌，因此，对于哺乳期妇女，ONGLYZA™应慎用。 儿童患者：尚未开展ONGLYZA™（沙格列汀saxagliptin）在儿童患者中的安全性和有效性研究。 Onglyza PRINCETON, N.J. & LONDON--(BUSINESS WIRE)--Bristol-Myers Squibb Company (NYSE: BMY) and AstraZeneca (NYSE: AZN) today announced that the U.S. Food and Drug Administration (FDA) approved ONGLYZA™ (saxagliptin), a dipeptidyl peptidase-4 (DPP4) inhibitor. ONGLYZA is indicated as an adjunct to diet and exercise to improve blood sugar (glycemic) control in adults for the treatment of type 2 diabetes mellitus. ONGLYZA once daily can be used in combination with commonly prescribed oral anti-diabetic medications – metformin, sulfonylureas or thiazolidinediones (TZD) – or as a monotherapy to significantly reduce glycosylated hemoglobin (A1C) levels. ONGLYZA should not be used for the treatment of type 1 diabetes or for the treatment of diabetic ketoacidosis (high levels of certain acids, known as ketones, in the blood or urine). ONGLYZA has not been studied in combination with insulin. “The FDA approval of ONGLYZA is an important development for adult patients with type 2 diabetes struggling every day to control their blood sugar levels. Nearly half of adult patients remain uncontrolled on their current treatment regimen and may thus require additional medications,” said Elliott Sigal, M.D., Ph.D, executive vice president, chief scientific officer, and president, Research & Development, Bristol-Myers Squibb. “Our ongoing clinical trial program has demonstrated that ONGLYZA showed improved A1C control both in combination and monotherapy settings.” “Type 2 diabetes is a daily challenge for adult patients and physicians. With the FDA approval of ONGLYZA, physicians and adult patients with type 2 diabetes have an important new treatment to help improve glucose control,” said David Brennan, chief executive officer, AstraZeneca. “ONGLYZA is the product of a major collaboration between AstraZeneca and Bristol-Myers Squibb to further the understanding of how best to treat this challenging disease and help adult patients achieve their treatment goals.” ONGLYZA™ (saxagliptin) Clinical Development Program The approval is based on a clinical development program, which included approximately 5,000 individuals, more than 4,000 of whom received ONGLYZA. As part of the development program, ONGLYZA, with diet and exercise, was studied as add-on therapy with other oral anti-diabetic medications, including metformin, the sulfonylurea glyburide and TZDs; in adult patients new to diabetes therapy starting metformin and ONGLYZA together; and as a monotherapy. Throughout the Phase III development program, treatment with ONGLYZA at all doses produced clinically relevant and statistically significant reductions in all three key measures of glucose control studied – A1C, fasting plasma glucose (FPG) and post-prandial glucose (PPG) – when partnered with other commonly used oral anti-diabetic agents (metformin, sulfonylureas and TZDs), or when used as a monotherapy. ONGLYZA was weight and lipid neutral compared to placebo. ONGLYZA Provides A1C Control Through Effects on Both FPG and PPG Incretin hormones help the body regulate glucose levels in response to meals by influencing the pancreatic secretion of insulin and glucagon. ONGLYZA increases and prolongs the action of incretin hormones by inhibiting the DPP4 enzyme that inactivates incretins usually within minutes. The inhibition of the DPP4 enzyme by ONGLYZA results in an increase in the production of insulin and a decrease in the production of glucagon by the pancreas. These effects are glucose dependent and enhance the body’s natural response to food to reduce blood sugar levels before and after meals. “I continue to see adult patients in my practice who, despite treatment, still have high FPG or high PPG, both of which are key contributors to elevated A1C," said Robert Henry, M.D., Chief, Endocrinology & Metabolism, University of California, San Diego. "The approval of saxagliptin provides a new treatment for adult patients with type 2 diabetes that helps to reduce A1C levels by working across key glucose measures to improve glycemic control.” ONGLYZA Complements Metformin to Provide Statistically Significant A1C Reductions ONGLYZA was studied extensively with metformin, the most commonly-prescribed oral anti-diabetic medication. In adult patients inadequately controlled on metformin, the addition of ONGLYZA 2.5 mg (n=192, baseline A1C 8.1 percent) and 5 mg (n=191, baseline A1C 8.1 percent) once daily reduced A1C levels from baseline to Week 24 by -0.6 percent and –0.7 percent respectively for ONGLYZA™ (saxagliptin) vs. +0.1 percent increase for placebo (p<0.0001 vs. placebo, n=179, baseline A1C 8.1 percent). The reported incidence of hypoglycemia in ONGLYZA 2.5 mg and 5 mg compared with placebo was 7.8 percent, 5.8 percent and 5 percent, respectively. For those new to diabetes medications, the use of ONGLYZA 5 mg with metformin (n=320, baseline A1C 9.4 percent) as initial therapy lowered A1C from baseline to week 24 by -2.5 percent vs. -2 percent for metformin plus placebo (p<0.0001, n=313, baseline A1C 9.4 percent). Significantly more adult patients in the ONGLYZA plus metformin arm achieved the American Diabetes Association recommended A1C level of less than 7 percent than those treated with metformin plus placebo (60 percent vs. 41 percent, respectively, p<0.05). The reported incidence of hypoglycemia was 3.4 percent in adult patients given ONGLYZA 5 mg plus metformin and 4 percent in adult patients given metformin alone. The adverse reactions occurring in ≥5 percent of adult patients and more commonly than in adult patients treated with metformin alone were headache (7.5 percent vs. 5.2 percent) and nasopharyngitis (6.9 percent vs. 4 percent). Complementary and Statistically Significant A1C Reductions When Added to the Sulfonylurea Glyburide or TZDs ONGLYZA also offered better glucose control for adult patients currently uncontrolled on glyburide. The addition of ONGLYZA 2.5 mg (n=248, baseline A1C 8.4 percent) or 5 mg (n=253, baseline A1C 8.5 percent) to a submaximal total daily dose of glyburide 7.5 mg reduced A1C levels from baseline at week 24 by -0.5 percent and -0.6 percent, respectively for ONGLYZA vs. +0.1 percent increase with an approximate doubling of the total daily dose of the glyburide plus placebo (p<0.0001 vs. uptitrated glyburide, n=267, baseline A1C 8.4 percent). The reported incidence of hypoglycemia for ONGLYZA 2.5 mg or 5 mg compared with the high-dose glyburide group was 13.3 percent and 14.6 percent vs. 10.1 percent, respectively. Confirmed hypoglycemia was 2.4 percent, 0.8 percent and 0.7 percent, respectively (defined as symptoms of hypoglycemia accompanied by a fingerstick glucose value of ≤50 mg/dL). When used with a sulfonylurea, a lower dose of the sulfonylurea may be required to reduce the risk of hypoglycemia. When used in addition to TZDs (pioglitazone or rosiglitazone), ONGLYZA™ (saxagliptin) offered additional glucose control. The addition of ONGLYZA 2.5 mg (n=195, baseline A1C 8.3 percent) and 5 mg (n=186, baseline A1C 8.4 percent) reduced A1C levels from baseline at week 24 by -0.7 percent and -0.9 percent, respectively vs. –0.3 percent for placebo (p<0.05 vs. placebo, n=184, baseline A1C 8.2 percent). The reported incidence of hypoglycemia with ONGLYZA 2.5 mg and 5 mg compared with placebo was 4.1 percent and 2.7 percent vs. 3.8 percent, respectively. The incidence of peripheral edema was 3.1 percent and 8.1 percent vs. 4.3 percent as compared to placebo; none resulted in discontinuation of therapy. ONGLYZA Provides Significant A1C Reduction When Used as Monotherapy When studied as a monotherapy, ONGLYZA significantly improved glucose control, with a difference in A1C from baseline of -0.4 percent and -0.5 percent for ONGLYZA 2.5 mg (n=102, baseline A1C 7.9 percent) and 5 mg (n=106, baseline A1C 8.0 percent), respectively, vs. +0.2 percent increase for placebo (p<0.0001 vs. placebo, n=95, baseline A1C 7.9 percent) at Week 24. The reported incidence of hypoglycemia in the ONGLYZA groups compared with placebo given as monotherapy was 4 percent and 5.6 percent vs. 4.1 percent, respectively. ONGLYZA had an Overall Incidence of Side Effects Similar to Placebo In clinical trials, the overall incidence of side effects for ONGLYZA 2.5 mg and 5 mg was similar to placebo (72 percent and 72.2 percent vs. 70.6 percent, respectively). The most common events reported with ONGLYZA 5 mg (≥5 percent and more commonly than placebo) were upper respiratory tract infection (7.7 percent vs. 7.6 percent, respectively), urinary tract infection (6.8 percent vs. 6.1 percent, respectively) and headache (6.5 percent vs. 5.9 percent, respectively). In adult patients treated with ONGLYZA 2.5 mg, only headache (6.5 percent) was reported at ≥5 percent and more commonly than in adult patients treated with placebo. Discontinuation of therapy due to adverse events occurred in 2.2 percent, 3.3 percent, and 1.8 percent of patients receiving ONGLYZA 2.5 mg, ONGLYZA 5 mg, and placebo, respectively. There was a dose-related mean decrease in absolute lymphocyte count observed with ONGLYZA. ONGLYZA™ (saxagliptin) Offers Convenient Once Daily Dosing ONGLYZA offers convenient, once-daily dosing of 2.5 mg or 5 mg that can be taken regardless of meals. ONGLYZA 2.5 mg is recommended for adult patients with moderate or severe renal impairment, or end-stage renal disease requiring hemodialysis (creatinine clearance less ≤50 mL/min). ONGLYZA has not been studied in patients undergoing peritoneal dialysis. Assessment of renal function is recommended prior to initiation of ONGLYZA and periodically thereafter. The dose for ONGLYZA should be limited to 2.5 mg when coadministered with strong cytochrome P450 3A4/5 (CYP 3A4/5) inhibitors (e.g., ketoconazole). No dose adjustment is required based on gender, race, weight or hepatic impairment. IMPORTANT INFORMATION ABOUT ONGLYZA Indication and Important Limitations of Use ONGLYZA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. ONGLYZA should not be used for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis. ONGLYZA has not been studied in combination with insulin. Important Safety Information Use With Medications Known to Cause Hypoglycemia: Insulin secretagogues, such as sulfonylureas, cause hypoglycemia. Therefore, a lower dose of the insulin secretagogue may be required to reduce the risk of hypoglycemia when used in combination with ONGLYZA. Drug Interactions: Because ketoconazole, a strong CYP 3A4/5 inhibitor, increased saxagliptin exposure, the dose of ONGLYZA should be limited to 2.5 mg when coadministered with a strong CYP 3A4/5 inhibitor (e.g., atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin). Patients with Renal Impairment: The dose of ONGLYZA is 2.5 mg once daily for patients with moderate or severe renal impairment, or with end-stage renal disease requiring hemodialysis (creatinine clearance ≤50 mL/min). ONGLYZA should be administered following hemodialysis. ONGLYZA has not been studied in patients undergoing peritoneal dialysis. Assessment of renal function is recommended prior to initiation of ONGLYZA and periodically thereafter. Pregnant and Nursing Women: There are no adequate and well-controlled studies in pregnant women. ONGLYZA, like other antidiabetic medications, should be used during pregnancy only if clearly needed. It is not known whether saxagliptin is secreted in human milk. Because many drugs are secreted in human milk, caution should be exercised when ONGLYZA is administered to a nursing woman. Pediatric Patients: Safety and effectiveness of ONGLYZA™ (saxagliptin) in pediatric patients have not been established. Bristol-Myers Squibb and AstraZeneca Collaboration Bristol-Myers Squibb and AstraZeneca entered into a collaboration in January 2007 to enable the companies to research, develop and commercialize select investigational drugs for type 2 diabetes. The Bristol-Myers Squibb/AstraZeneca Diabetes collaboration is dedicated to global patient care, improving patient outcomes and creating a new vision for the treatment of type 2 diabetes. About Bristol-Myers Squibb Bristol-Myers Squibb is a global biopharmaceutical company whose mission is to extend and enhance human life. For more information, visit www.bms.com. About AstraZeneca AstraZeneca is a major international healthcare business engaged in the research, development, manufacturing and marketing of prescription medicines and supplier for healthcare services. AstraZeneca is one of the world's leading pharmaceutical companies with healthcare sales of US$ 31.6 billion and is a leader in gastrointestinal, cardiovascular, neuroscience, respiratory, oncology and infectious disease medicines. For more information about AstraZeneca, please visit: www.astrazeneca.com ONGLYZA is a trademark of the Bristol-Myers Squibb Company.
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盐酸沙格列汀片|ONGLYZA（SAXAGLIPTIN HYDROCHLORIDE）简介：
商品名：Onglyza
通用名：Saxagliptin沙格列汀
Saxagliptin为白色到淡黄色或者淡棕色，非吸湿性，结晶性粉末。在24°C ± 3°C水中难溶，乙酸乙酯微溶，溶于甲醇，乙醇，异丙醇，乙腈，丙酮， ... 责任编辑：admin |
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