• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

特索格列净:一种长效人胰高血糖素样肽-1 类似物。

Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue.

机构信息

Rikshospitalet-Oslo University Hospital, Lipid Clinic, Medical Department, 0027 Oslo, Norway.

出版信息

Expert Opin Investig Drugs. 2009 Sep;18(9):1405-11. doi: 10.1517/13543780903164205.

DOI:10.1517/13543780903164205
PMID:19678802
Abstract

BACKGROUND

Taspoglutide (R1583/BIM51077) is a new anti diabetic drug from Hoffmann-La Roche. The compound is to be administered as a subcutaneous injection once weekly and is also effective given bi-weekly. It is a long acting 10% formulation of (Aib 8-35) human glucagon-like polypeptide-1 (7 - 36 amides) with 93% homology with the native polypeptide. It activates the glucagon-like polypeptide-1 receptor. Phase III trials are currently in process.

OBJECTIVE

To provide a critical review of taspoglutide based on available published data.

METHODS

Information provided from the search on Internet has been reviewed. A clinical interpretation is given on a background of practical experience as an investigator in a clinical trial with taspoglutide.

RESULTS

Search on PubMed, EMBASE and Google gave hits on six clinical studies investigating taspoglutide of which the largest accounted for > 50% of the total study population. In addition, some animal studies were identified. Significant improvement on glucose control as well as several metabolic parameters has been shown with taspoglutide.

DISCUSSION

Data from the clinical trials are interpreted in a medical context. The prospects of taspoglutide in the treatment of diabetes type 2 and metabolic syndrome are discussed.

CONCLUSION

Taspoglutide is a new activator of the glucagon-like polypeptide-1 receptor. It is effective when injected once weekly and less effective when injected bi-weekly. In addition to its anti diabetic properties, taspoglutide has favorable effects on body weight and significantly reduces three of five diagnostic criteria for metabolic syndrome, namely glucose, waist circumference and fasting triglyceride.

摘要

背景

Taspoglutide(R1583/BIM51077)是罗氏制药的一种新型抗糖尿病药物。该化合物通过皮下注射给药,每周一次,每两周一次也同样有效。它是一种长效 10%的(Aib8-35)人胰高血糖素样肽-1(7-36 酰胺)制剂,与天然多肽有 93%的同源性。它能激活胰高血糖素样肽-1 受体。目前正在进行 III 期临床试验。

目的

基于现有已发表的数据,对 taspoglutide 进行批判性评价。

方法

检索互联网上提供的信息,并结合作为 taspoglutide 临床试验研究者的实际经验进行临床解读。

结果

在 PubMed、EMBASE 和 Google 上搜索到 6 项研究 taspoglutide 的临床试验,其中最大的一项研究占总研究人群的 50%以上。此外,还确定了一些动物研究。研究表明,taspoglutide 能显著改善血糖控制和多种代谢参数。

讨论

对临床试验数据进行医学背景下的解读。讨论了 taspoglutide 在治疗 2 型糖尿病和代谢综合征方面的前景。

结论

Taspoglutide 是一种新型胰高血糖素样肽-1 受体激动剂。每周注射一次有效,每两周注射一次效果较差。除了抗糖尿病作用外,taspoglutide 还对体重有有利影响,并显著降低了代谢综合征的五个诊断标准中的三个,即血糖、腰围和空腹甘油三酯。

相似文献

1
Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue.特索格列净:一种长效人胰高血糖素样肽-1 类似物。
Expert Opin Investig Drugs. 2009 Sep;18(9):1405-11. doi: 10.1517/13543780903164205.
2
Safety and tolerability of high doses of taspoglutide, a once-weekly human GLP-1 analogue, in diabetic patients treated with metformin: a randomized double-blind placebo-controlled study.在接受二甲双胍治疗的糖尿病患者中,高剂量每周一次人胰高血糖素样肽-1 类似物 taspoglutide 的安全性和耐受性:一项随机、双盲、安慰剂对照研究。
Diabet Med. 2010 May;27(5):556-62. doi: 10.1111/j.1464-5491.2010.02990.x.
3
Clinical efficacy and safety of once-weekly glucagon-like peptide-1 agonists in development for treatment of type 2 diabetes mellitus in adults.正在开发中的每周一次胰高血糖素样肽-1 激动剂治疗成人 2 型糖尿病的临床疗效和安全性。
Ann Pharmacother. 2012 Jan;46(1):68-78. doi: 10.1345/aph.1Q379.
4
An overview of once-weekly glucagon-like peptide-1 receptor agonists--available efficacy and safety data and perspectives for the future.每周一次胰高血糖素样肽-1 受体激动剂概述——现有疗效和安全性数据及未来展望。
Diabetes Obes Metab. 2011 May;13(5):394-407. doi: 10.1111/j.1463-1326.2011.01357.x. Epub 2011 Jan 5.
5
Efficacy and safety of long-acting glucagon-like peptide-1 receptor agonists compared with exenatide twice daily and sitagliptin in type 2 diabetes mellitus: a systematic review and meta-analysis.长效胰高血糖素样肽-1 受体激动剂与艾塞那肽每日 2 次和西格列汀在 2 型糖尿病中的疗效和安全性比较:系统评价和荟萃分析。
Ann Pharmacother. 2011 Jul;45(7-8):850-60. doi: 10.1345/aph.1Q024. Epub 2011 Jul 5.
6
Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis.胰高血糖素样肽-1受体激动剂在2型糖尿病治疗中的疗效与安全性:一项系统评价和混合治疗比较分析
Diabetes Obes Metab. 2017 Apr;19(4):524-536. doi: 10.1111/dom.12849. Epub 2017 Feb 17.
7
Taspoglutide, a novel human once-weekly analogue of glucagon-like peptide-1, improves glucose homeostasis and body weight in the Zucker diabetic fatty rat.塔斯格鲁肽,一种新型人胰高血糖素样肽-1 类似物,可改善 Zucker 糖尿病肥胖大鼠的葡萄糖稳态和体重。
Diabetes Obes Metab. 2010 Aug;12(8):674-82. doi: 10.1111/j.1463-1326.2010.01207.x.
8
A direct comparison of long- and short-acting GLP-1 receptor agonists (taspoglutide once weekly and exenatide twice daily) on postprandial metabolism after 24 weeks of treatment.长效和短效胰高血糖素样肽-1受体激动剂(每周一次的塔司鲁肽和每日两次的艾塞那肽)治疗24周后对餐后代谢的直接比较。
Diabetes Obes Metab. 2014 Feb;16(2):170-8. doi: 10.1111/dom.12192. Epub 2013 Aug 22.
9
The fate of taspoglutide, a weekly GLP-1 receptor agonist, versus twice-daily exenatide for type 2 diabetes: the T-emerge 2 trial.每周一次 GLP-1 受体激动剂替西帕肽与每日两次艾塞那肽治疗 2 型糖尿病的结局:T-emerge 2 试验。
Diabetes Care. 2013 Mar;36(3):498-504. doi: 10.2337/dc12-0709. Epub 2012 Nov 8.
10
Taspoglutide, a once-weekly glucagon-like peptide 1 analogue, vs. insulin glargine titrated to target in patients with Type 2 diabetes: an open-label randomized trial.特索格列净,一种每周一次的胰高血糖素样肽 1 类似物,与根据目标调整剂量的甘精胰岛素治疗 2 型糖尿病患者的比较:一项开放标签随机试验。
Diabet Med. 2013 Jan;30(1):109-13. doi: 10.1111/dme.12003.

引用本文的文献

1
Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes.胰高血糖素样肽-1及其B类G蛋白偶联受体:通往治疗成功的漫长征程。
Pharmacol Rev. 2016 Oct;68(4):954-1013. doi: 10.1124/pr.115.011395.
2
Glucagon-like peptide-1 receptor agonists versus insulin glargine for type 2 diabetes mellitus: A systematic review and meta-analysis of randomized controlled trials.胰高血糖素样肽-1受体激动剂与甘精胰岛素治疗2型糖尿病的疗效比较:一项随机对照试验的系统评价和荟萃分析
Curr Ther Res Clin Exp. 2010 Aug;71(4):211-38. doi: 10.1016/j.curtheres.2010.08.003.
3
Impact of GLP-1 receptor agonists on major gastrointestinal disorders for type 2 diabetes mellitus: a mixed treatment comparison meta-analysis.
胰高血糖素样肽-1受体激动剂对2型糖尿病主要胃肠道疾病的影响:一项混合治疗比较荟萃分析。
Exp Diabetes Res. 2012;2012:230624. doi: 10.1155/2012/230624. Epub 2012 Dec 26.
4
Efficacy and safety of taspoglutide monotherapy in drug-naive type 2 diabetic patients after 24 weeks of treatment: results of a randomized, double-blind, placebo-controlled phase 3 study (T-emerge 1).在 24 周治疗后,初治 2 型糖尿病患者中单用替西帕肽的疗效和安全性:一项随机、双盲、安慰剂对照的 3 期研究(T-emerge 1)的结果。
Diabetes Care. 2012 Mar;35(3):485-7. doi: 10.2337/dc11-1942. Epub 2012 Feb 1.
5
Incretin therapy--present and future.肠促胰岛素疗法——现状与未来。
Rev Diabet Stud. 2011 Fall;8(3):307-22. doi: 10.1900/RDS.2011.8.307. Epub 2011 Nov 10.
6
Incretin-based therapy: a powerful and promising weapon in the treatment of type 2 diabetes mellitus.基于肠促胰岛素的治疗:治疗 2 型糖尿病的有力且有前景的武器。
Diabetes Ther. 2011 May;2(2):101-21. doi: 10.1007/s13300-011-0002-3. Epub 2011 Feb 28.
7
Glucagon-like peptide-1 analogues for Type 2 diabetes mellitus: current and emerging agents.胰高血糖素样肽-1 类似物治疗 2 型糖尿病:现有及新兴药物。
Drugs. 2011 Sep 10;71(13):1675-88. doi: 10.2165/11592810-000000000-00000.
8
The evolving place of incretin-based therapies in type 2 diabetes.2 型糖尿病中肠促胰岛素治疗的不断发展。
Pediatr Nephrol. 2010 Jul;25(7):1207-17. doi: 10.1007/s00467-009-1435-z. Epub 2010 Feb 4.