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  药店国别: 瑞士药房
产地国家: 瑞士
所属类别: 糖尿病->2型糖尿病
处方药:处方药
包装规格: 50毫克/片 112片/盒
计价单位:
  点击放大  
生产厂家中文参考译名:
诺华
生产厂家英文名:
Novartis
该药品相关信息网址1:
http://www.medicines.org.uk/guides/galvus/Diabetes/
该药品相关信息网址2:
http://www.netdoctor.co.uk/diabetes/medicines/galvus.html
原产地英文商品名:
Galvus 50mg/tab 112tabs/box
原产地英文药品名:
vildagliptin
中文参考商品译名:
Galvus 50毫克/片 112片/盒
中文参考药品译名:
维达列汀
中文参考化合物名称:
1-[[(3一羟基一l一金刚烷基)氨基]乙酰基]-2-氰基一(5)-四氢吡咯烷
原产地国家批准上市年份:
2007/09/28
英文适应病症1:
diabetes
英文适应病症2:
Type 2 diabetes
临床试验期:
完成
中文适应病症参考翻译1:
糖尿病
中文适应病症参考翻译2:
2型糖尿病
药品信息:

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 详细处方信息以本药内容附件PDF文件(201221618174215.pdf)的“原文Priscribing Information”为准
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部分中文维达列汀处方资料(仅供参考)

2007年9月28日,诺华公司宣布其口服抗糖尿病新药维达列汀(vildagliptin,商品名:Galvus)获得欧盟委员会批准,将在27个欧盟国家及挪威和爱尔兰上市。其化学名为1-[[(3一羟基一l一金刚烷基)氨基]乙酰基]-2-氰基一(5)-四氢吡咯烷,分子式为c17H15N3O2,相对分子质量为303.4。本品与默克公司2006年FDA批准上市的西他列汀(sitagliptin,Januvia)同属IV型二肽基肽酶(DPP_4)抑制剂。

l药理作用
本品是一种具有选择性、竞争性、可逆的DPP_4抑制剂。葡萄糖依赖性促胰岛素多肽(GIP)和胰高血糖素样多肽.1(GLP.1)是维持体内葡萄糖浓度的重要激素,都具有肠促胰岛素作用。2型糖尿病患者GIP的促胰岛素分泌作用受损,仅有GLP·l能发挥促胰岛激素分泌作用,它通过作用于胰岛B细胞膜上的受体,促进胰岛素的分泌。GLP.1还可抑制胰高fliL糖素的分泌以及抑制胃排空从而增加饱足感(抑制食欲)。DPP4与蛋白结合存在于许多组织中,如肾、肝、小肠膜的刷状边缘、胰管、淋巴细胞、内皮细胞,其能通过水解GLP-1的N端第2位丙氨酸迅速使其失活。
本品通过与DPP一4结合形成DPP一4复合物而抑制该酶的活性,在提高GLP-l浓度,促使胰岛B细胞产生胰岛素的同时,降低胰高血糖素浓度,从而降低血糖。且对体重无明显影响。

2药动学
健康人体药动学研究表明,口服本品吸收迅速,生物利用度约为85%。达峰时间为给药后1—2h,血浆半衰期为1.5—4.5h,蛋白结合率低(4%~17%)。其体内过程具有线性药动学特征,多次口服给药后未出现药物蓄积,其药动学参数不受食物影响。
本品代谢途径较多,大部分药物(55%)通过肝水解(氰基水解)灭活,主要代谢产物LAYl51无药理活性。很少一部分母体药物由CYP450酶系统代谢。本品主要通过尿排泄,尿中含有18%一22%的原型药物。
单次服用本品(25~200mg)可迅速抑制血浆中DPP.4活性,30~60min可抑制90%DPP4的活性。DPP-4抑制作用持续时间具有剂量依耐性,口服50和loomg本品后,12h内DPP4活性抑制可分别达70%和90%;口服100mg,24h仍可抑制40%的DPP4活性。肝功能异常患者使用本品无需调整剂量。

3临床研究
3.1单药治疗
Pratley等评估2型糖尿病患者单用本品治疗12周的疗效。纳入标准:年龄≥30岁,且先期仅通过饮食控制,空腹血糖浓度1.1—2.7g-L“(6.1一15mmo卜L。1),糖基化血红蛋白(HbAh)值6.8%一11%,体重指数(BMI)为20一40kg·m~。随机分为本品25mg,bid组(凡=70)和安慰剂组(n=28),口服给药。结果:12周后,本品组对脂水平无影响,空腹及餐后血糖浓度都显著下降,同时提高了B细胞的功能,且未引起体重的改变。两组在体重上无显著差异,不良反应发生率相似。
在另一个12周的双盲、剂量效应试验中,Ristic等评估了本品对HbA。。的作用效果、安全性以及耐受性。患者随机分为5组:本品25mg(qd)组(乃=51),25mg(bid)组(,I=54),50mg(qd)组(n=53),100mg(qd)组(,l=63)及安慰剂组(n=58).。结果表明,本品50mg和100mg(qd)组能有效降低HbA。值,且100mg(qd)组B细胞功能(B细胞分泌功能指数,HOMA—B)显著提高,并显示出良好的安全性和耐受性。表明更高剂量的本品降血糖作用可能与B细胞功能的提高有关。各组不良反应的发生率相似。
3.2联合用药
3.2.1与二甲双胍联用¨叫在一个随机、双盲、多中心对照试验中,纳入标准为:持续使用二甲双胍(剂量≥l500mg·d一)且血糖控制并不理想[HbA。。7.5%一11%]的2型糖尿病患者,分为3组:二甲双胍联合本品50mg·d“组(n=177)和100mg-dil组(n=185),二甲双胍联合安慰剂组(,l=182),治疗24周。结果表明:应用二甲双胍未能很好控制血糖的2型糖尿病患者加用本品能使空腹血糖和AIc均呈剂量相关性地降低,且耐受性良好。
另一项52周的研究评价了本品对B细胞功能的影响。2型糖尿病患者随机分为两组:本品(50mg,qd)联合二甲双胍组(n=31),安慰剂联合二甲双胍组(,l=26),二甲双胍剂量为1.5—3.0mg-d~。通过计算适应指数(评价p细胞功能敏感性的参数)评价B细胞功能。结果表明本品联合二甲双胍能提高2型糖尿病患者的B细胞功能及餐后胰岛素的敏感度。
3.2.2与匹格列酮联用
一个24周多中心、随机双盲对照试验研究考察了本品与匹格列酮联合应用的有效性和耐受性。纳入463例先前单独使用匹格列酮(45mg·d。1)控制血糖无效的2型糖尿病患者,在加用本品(50或100mg·d。)和安慰剂后通过协变量分析的模式进行有效性参数分析。结果与安慰剂相比,本品两种剂量均能显著增加胰岛素的释放率。表明:本品与最大剂量的匹格列酮联用仍有效,耐受性良好,且并未增加低血糖的发生率。3.2.3与胰岛素联用¨引一个24周、多中心、随机双盲临床试验中,纳入使用胰岛素(>30u·d“)治疗,且HbA,,值为7.5%一11%,在试验前3个月内未使用口服抗糖尿病药物的2型糖尿病患者,试验期间胰岛素剂量允许调整。随机分为两组:联合本品50mg(bid)治疗组(凡=125)和安慰剂治疗组(n=131)。结果表明:2型糖尿病患者特别是老年患者,尽管出现临床胰岛素抵抗,应用胰岛素联合本品能显著降低HbA,,值,且低血糖的发生率及严重性显著低于单用胰岛素,这可能与p细胞功能的改善有关,尚需进一步研究。

4不良反应和药物相互作用
本品最常见的不良反应有头痛、鼻咽炎、咳嗽、便秘、头晕和增加出汗量等。低血糖的发生率与安慰剂相似。
Colleen等副报道,格列本脲10mg·d一与本品100mg(bid)联合服用28d,并无药物代谢方面的相互作用,且无低血糖报道。此外评估了吡格列酮45mg·d“和本品100mg·d。联合使用28d的安全性和药动学,通过测定联合治疗前与治疗期间吡格列酮和本品的血药浓度,发现两种药物的血药浓度在任何时间点均无显著改变。表明格列本脲或吡格列酮与本品联合应用都是安全的。
本品在临床试验中显示了相对的安全性,但DPP4酶存在于很多组织中,它作为人体多种激素和肽的酶作用底物,其长期抑制是否对这些物质有影响,还需进一步研究。

5结语
综上所述,本品具有降低HbA1c、空腹及餐后血糖水平、餐后胰高血糖素分泌及提高B细胞功能的作用,为2型糖尿病患者的治疗提供了新选择。该药与其他药物联合使用的安全性和有效性,禁忌证、不良反应等还有待于更多的临床研究观察。

Galvus (vildagliptin) - DPP-IV Inhibitor / Oral
Novartis' Galvus (vildagliptin) is a member of a new class of oral antidiabetic agents known as dipeptidyl peptidase IV inhibitors (DPP-IV) inhibitors or 'incretin enhancers'. Its mode of action is distinct from established antidiabetic medications and appears to include disease-modifying effects in patients with type 2 diabetes.

Galvus (vildagliptin), in advanced-stage development as a treatment for patients with type 2 diabetes, has now received the thumbs up from regulators in Europe. The EMEA has approved its use in combination with other anti-diabetic medications including metformin, sulfonylureas and thiazolidinediones. Approval has also been granted for Eucreas, a single tablet formulation of Galvus (vildagliptin) and metformin.

In March 2006, a new drug application for Galvus was accepted for review by the FDA. In February 2007, the FDA requested Novartis to conduct a new study to assess the safety and efficacy of Galvus in patients with impaired kidneys.

Novartis submitted data based on this request in November 2007. The data, however, showed frequent enzyme elevation levels in patients taking higher doses of Galvus. Due to safety concerns, the approval of Galvus was further delayed by the FDA.

In January 2008, Novartis said that the company might not refile for the approval of Galvus until it receives clarification on the kind of data required by the FDA for the drug approval. Following this development, the approval of Galvus in the US remains uncertain. Galvus is, however, presently approved in 70 countries and has been launched in 37 countries.

DPP-IV inhibition – diabetes treatment
Glucagon-like peptide-1 (GLP-1) and gastric inhibitor peptide (GIP) are naturally occurring hormones (incretins) that are released from cells in the gut in response to food. They bind to receptors on pancreatic beta cells stimulating the release of the hormone insulin, responsible for the regulation of blood sugar levels.

GLP-1 also reduces the secretion of glugacon, a hormone produced by the pancreas that stimulates the liver to convert glycogen to glucose, thus increasing blood sugar levels. Naturally produced GLP-1 has a very short half-life of less than two minutes.

Patients with type 2 diabetes have impaired incretin function and are thus unable to properly regulate their blood sugar levels, which can lead to adverse clinical sequelae. Novartis' Galvus (vildagliptin) works by inhibiting DPP-IV, an enzyme that breaks down GLP-1.

By delaying the degradation of GLP-1, vildagliptin extends the action of insulin while also suppressing the release of glucagon. This leads to a reduction in elevated blood glucose levels (hyperglycaemia), which is a characteristic feature of type 2 diabetes.

Galvus effective in type 2 diabetics
Administration of Galvus (vildagliptin) to patients with type 2 diabetes suggests it is a safe and effective treatment with the potential to achieve long-term glycaemic control, a recognised deficiency of current oral anti-diabetic medications.

In phase II trials the addition of vildagliptin 50mg/day to metformin, a standard treatment for type 2 diabetes, resulted in improved glucose control in patients inadequately controlled on metformin alone. Levels of haemoglobin A1c (HbA1c), fasting plasma glucose, mean prandial glucose and peak prandial glucose were reduced to a significantly greater effect after 12 weeks of additional treatment with vildagliptin compared with continued therapy with metformin alone.

Importantly, the results achieved at 12 weeks were sustained over a year, indicating that patients treated with vildagliptin can achieve good long-term glycaemic control. In patients maintained on metformin alone, glycaemic control tended to deteriorate over time.

Long-term treatment with Galvus (vildagliptin) appears well tolerated as reflected by low rates of study discontinuation for adverse events in clinical trials. In the phase II trials, drug-related adverse events occurred in 4.8% of patients receiving vildagliptin in addition to metformin compared with 6.9% of those receiving metformin plus the placebo. Treatment with vildagliptin does not appear associated with weight gain, which is an important benefit for patients with type 2 diabetes.

In phase III trials Galvus (vildagliptin) has been evaluated as both monotherapy and in combination with other standard antidiabetic drugs.

Potential to preserve pancreatic beta cell function
Patients with type 2 diabetes experience the progressive loss of pancreatic beta cell function and a concomitant loss of insulin secretion and glycaemic control. In preclinical studies, Galvus (vildagliptin) was found to have a beneficial effect on insulin secretion by increasing beta cell production and inhibiting programmed cell death (apoptosis).

Subsequent clinical studies, in which vildagliptin was administered to patients with type 2 diabetes not previously treated with oral antidiabetic medications, showed that it increased the active forms of GLP-1 and GIP when compared with the placebo. This translated into improved beta cell function as measured by enhanced insulin secretion on glucose challenge.

The drug's ability to improve the functioning of insulin-producing cells in the pancreas, albeit in studies with small numbers of patients, suggests it may have disease-modifying potential in the treatment of type 2 diabetes.

Marketing commentary
The World Health Organization (WHO) estimates that globally over 170 million people have diabetes. Type 2 diabetes accounts for 90% to 95% of all cases of diabetes. The worldwide costs associated with treating diabetes and its complications are estimated to exceed $200bn a year.

By 2030 the prevalence of diabetes is predicted to double, driven by adverse lifestyle changes which have seen an explosion in the incidence of obesity, a risk factor for type 2 diabetes. Worldwide, diabetes is a huge and growing problem for which new treatments are needed.

DPP-IV inhibitors are one of several new classes of antidiabetic medications in development for type 2 diabetes. The ability to achieve sustainable reductions in HbA1c, the primary measure of blood glucose control, with an orally administered, well-tolerated agent is seen as one of the most important advantages of this new class of drugs.

Novartis' Galvus (vildagliptin) joins Merck's Januvia (sitagliptin) as the second DPP-IV inhibitor to secure regulatory approval. The US FDA approved the use of Januvia (sitagliptin) as new treatment for type 2 diabetics in October 2006.

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 详细处方信息以本药内容附件PDF文件(201221618174215.pdf)的“原文Priscribing Information”为准
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更新日期: 2014-07-30
附件:




201221618175622.pdf    

201221618174215.PDF    

 
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