{"title":"Albiglutide, an albumin-based fusion of glucagon-like peptide 1 for the potential treatment of type 2 diabetes.","authors":"Gerald H Tomkin","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>Albiglutide, under development by GlaxoSmithKline plc for the treatment of type 2 diabetes mellitus (T2DM), is an albumin-fusion peptide. The compound is a mimetic of glucagon-like peptide 1 (GLP-1), a hormone that decreases glucose levels, but has a short half-life because of degradation by dipeptidyl peptidase (DPP)-4. Albiglutide has a longer half-life as a result of its fusion with albumin and its resistance to degradation by DPP-4, caused by an amino acid substitution (Ala to Glu) at the DPP-4-sensitive hydrolysis site. Data from phase II clinical trials in patients with T2DM revealed that albiglutide was well tolerated and that the drug significantly reduced HbA1c levels compared with placebo. At the time of publication, phase III trials assessing albiglutide alone and in combination with other antidiabetic drugs were recruiting patients with T2DM. Albiglutide represents a promising new drug for the treatment of patients with T2DM; the results of long-term trials are awaited with interest.</p>","PeriodicalId":50605,"journal":{"name":"Current Opinion in Molecular Therapeutics","volume":"11 5","pages":"579-88"},"PeriodicalIF":0.0000,"publicationDate":"2009-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Opinion in Molecular Therapeutics","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
Albiglutide, under development by GlaxoSmithKline plc for the treatment of type 2 diabetes mellitus (T2DM), is an albumin-fusion peptide. The compound is a mimetic of glucagon-like peptide 1 (GLP-1), a hormone that decreases glucose levels, but has a short half-life because of degradation by dipeptidyl peptidase (DPP)-4. Albiglutide has a longer half-life as a result of its fusion with albumin and its resistance to degradation by DPP-4, caused by an amino acid substitution (Ala to Glu) at the DPP-4-sensitive hydrolysis site. Data from phase II clinical trials in patients with T2DM revealed that albiglutide was well tolerated and that the drug significantly reduced HbA1c levels compared with placebo. At the time of publication, phase III trials assessing albiglutide alone and in combination with other antidiabetic drugs were recruiting patients with T2DM. Albiglutide represents a promising new drug for the treatment of patients with T2DM; the results of long-term trials are awaited with interest.
Albiglutide是一种白蛋白融合肽,由葛兰素史克公司开发,用于治疗2型糖尿病(T2DM)。该化合物是胰高血糖素样肽1 (GLP-1)的模拟物,胰高血糖素样肽1是一种降低葡萄糖水平的激素,但由于被二肽基肽酶(DPP)-4降解,半衰期短。Albiglutide具有较长的半衰期,这是因为它与白蛋白融合,并且由于DPP-4敏感水解位点的氨基酸取代(Ala to Glu),它对DPP-4的降解具有抵抗力。来自T2DM患者的II期临床试验数据显示,阿比鲁肽耐受性良好,与安慰剂相比,该药可显著降低HbA1c水平。在本文发表时,评估阿比鲁肽单独和与其他抗糖尿病药物联合使用的III期试验正在招募T2DM患者。阿比鲁肽是一种很有前途的治疗2型糖尿病的新药;人们饶有兴趣地等待着长期试验的结果。