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利拉鲁肽即将进入日本市场

 继日本中央社会保险医疗委员会批准了Victoza®(利拉鲁肽)的定价之后,诺和诺德制药公司计划将尽快在当地市场推出这种产品。诺和诺德表示,Victoza®是首个在日本获准上市的GLP-1类药物,既可以单独用药,也可以作为辅助药物与磺脲类降糖药(SU)联用。

Liraglutide, a once-daily human GLP-1 analogue

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发布日期:2010-05-12 16:23 文章来源:丁香园
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关键词: 诺和诺德 GLP-1 肠促胰素 利拉鲁肽   点击次数:

GLP-1类似物Liraglutide(利拉鲁肽)的作用可以持续24小时,每天仅需用药一次,能够提供类似于内源性GLP-1的生理效应,包括根据葡萄糖水平促进胰岛素分泌、抑制胰高糖素、延迟胃排空;在动物实验中,还能防止B细胞凋亡并促进其再生。

由于促进胰岛素分泌的作用是依赖于血糖水平的,因此发生低血糖的危险比较低。临床试验证实,Liraglutide能够降低空腹及餐后血糖,HbA1C水平能够降低1~2%;某些试验甚至表明,Liraglutide能够降低某些心血管风险的生物标记,明显降低甘油三酯的水平。

当然,还需要进行相关实验验证究竟Liraglutide能否改善2型糖尿病患者的进程。

Glucagon-like peptide-1 (GLP-1) is an incretin hormone physiologically playing a role in glucose homeostasis, together with the partner incretin,glucose dependent insulinotropic peptide (GIP). Active concentrations of this hormone are not maintained for long because of its very rapid degradation and elimination. The effects of the hormone are of potential therapeutic value in type 2 diabetes; therefore, analogues of GLP-1 have been developed that are characterised by a prolonged circulating half-life relative to the naturally occurring hormone. One such long-acting analogue is liraglutide.

The effects of liraglutide are maintained over 24 h, allowing once-daily dosing. Liraglutide provides all of the beneficial actions of endogenous GLP-1: glucose dependent stimulation of insulin secretion, glucagon suppression, deceleration of gastric emptying, appetite suppression/weight loss and, in animal models, inhibition of β-cell apoptosis and promotion of β-cell regeneration.Because liraglutide stimulates insulin secretion and suppresses glucagon secretion only when blood glucose levels are elevated, the risk of treatment-associated hypoglycaemia is low.

In clinical studies, liraglutide substantially lowered fasting and postprandial glucose concentrations, with an overall reduction in haemoglobin A1c of up to 1~2%. In some studies, liraglutide has decreased several biomarkers of cardiovascular risk and lowered triglyceride levels significantly.

Side effects most commonly are gastrointestinal symptoms; they are usually mild to moderate and resolve over time. Long-term clinical trials are needed to assess whether the effects of liraglutide on the β cell translate into a durable improvement in β-cell function and mass in patients with type 2 diabetes and, if so, whether this will slow or halt disease progression and help prevent complications.
 


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