Liraglutide: A once-daily human glucagon-like peptide-1 analogue for type 2 diabetes mellitus

2010 ◽  
Vol 67 (16) ◽  
pp. 1326-1336 ◽  
Author(s):  
David Joffe
2009 ◽  
Vol 43 (9) ◽  
pp. 1433-1444 ◽  
Author(s):  
Joshua J Neumiller ◽  
R Keith Campbell

Objective: To review the pharmacology, pharmacokinetics, efficacy, and safety of liraglutide, a glucagon-like peptide 1 (GLP-1) analog for the treatment of type 2 diabetes mellitus. Data Sources: A MEDLINE search (1966–May 2009) was conducted for English-language articles using the terms glucagon-like peptide 1, incretin mimetic, NN2211, and liraglutide. Abstracts presented at the American Diabetes Association and European Association for the Study of Diabetes annual meetings in 2006, 2007, and 2008 were also searched for relevant data. Study Selection and Data Extraction: Articles pertinent to the pharmacology, pharmacokinetics, efficacy, and safety of liraglutide were reviewed. Data Synthesis: Liraglutide is a GLP-1 analog with pharmacokinetic properties suitable for once-daily administration. Clinical trial data from large, controlled studies demonstrate the effectiveness of liraglutide in terms of hemoglobin A1c (A1C) reduction, reductions in body weight, and the drug's low risk for hypoglycemic events when used as monotherapy. Data also support benefits of liraglutide therapy on β-cell responsiveness to glucose, with animal and in vitro data indicating potential benefits in β-cell mass and neogenesis with liraglutide treatment. Liraglutide has been studied as monotherapy and in combination with metformin, glimepiride, and rosiglitazone for the treatment of type 2 diabetes. Additionally, comparative data with insulin glargine and exenatide therapy are available from Phase 3 trials providing practitioners valuable clinical data on which to base clinical decision making. Overall, liraglutide is well tolerated with dose-dependent nausea, vomiting, and diarrhea being the most commonly reported adverse events in clinical trials. Conclusions: Once-daily administration may provide a therapeutic advantage for liraglutide over twice-daily exenatide, with similar improvements in A1C and body weight observed when liraglutide was compared with exenatide. The glucose-dependent mechanism of insulin release with GLP-1 agonist therapy holds potential clinical significance in the management of postprandial hyperglycemic excursions, with minimal risk of hypoglycemia.


2018 ◽  
Vol 12 (4) ◽  
pp. 202-209 ◽  
Author(s):  
Spyridon N. Karras ◽  
Eleni Rapti ◽  
Theocharis Koufakis ◽  
Angeliki Kyriazou ◽  
Dimitrios G. Goulis ◽  
...  

2021 ◽  
Vol 37 (6) ◽  
pp. 74-83
Author(s):  
A.Yu. Gorbunova ◽  
E.P. Sannikova ◽  
I.I. Gubaidullin ◽  
O.M. Ignatova ◽  
M.Yu. Kopaeva ◽  
...  

In addition to the previously developed recombinant modified human glucagon-like peptide 1 (rmglp1, Glypin), a recombinant modified human glucose-dependent insulinotropic peptide (RMGIP) has been obtained. A new universal reverse-phase HPLC technique has been proposed allowing quantitative analysis of rmGlp1 and rmGip separately and as part of a two-component preparation. The data show that the design of recombinant human rmGip according to the Glypine formula makes it possible to produce one-component and two-component preparations containing various rmGip and rmGlp1 protein ratios ranging from 1:0 to 20:1, using cell biomass samples mixed in predetermined proportions. Studies of human rmGip activity in a mouse model revealed reduced specific activity and signs of weak antagonistic effects. In this regard, there is a need for further study of human rmGip activity in a mouse model, including the use of alternative mouse or rat rmGip. type 2 diabetes mellitus; two-component drug, glucose-dependent insulinotropic peptide, glucagon-like peptide-1 The work was supported by the Internal Grant from National Research Center Kurchatov Institute.


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