Research
Print page Print page
Switch language
The Capital Region of Denmark - a part of Copenhagen University Hospital
Published

Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus

Research output: Contribution to journalJournal articleResearchpeer-review

  1. Replacing SUs with incretin-based therapies for type 2 diabetes mellitus: challenges and feasibility

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Recent therapeutic advances in inflammatory bowel disease

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Digestive Disease Week 2001. Novel therapeutic principles in inflammatory bowel disease. 20-23 May 2001, Atlanta, GA, USA

    Research output: Contribution to journalJournal articleResearchpeer-review

  1. Investigating Intestinal Glucagon after Roux-en-Y Gastric Bypass Surgery

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Non-alcoholic fatty liver disease alters expression of genes governing hepatic nitrogen conversion

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Prognostic value of ratio of transmitral early filling velocity to early diastolic strain rate in patients with Type 2 diabetes

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. The Liver-α-Cell Axis and Type 2 Diabetes

    Research output: Contribution to journalReviewResearchpeer-review

  5. Evaluation of clinical translatability of the diet-induced obese and biopsy-confirmed gubra amylin mouse model of non-alcoholic steatohepatitis

    Research output: Contribution to journalConference abstract in journalResearchpeer-review

View graph of relations
Lixisenatide, under development by sanofi-aventis, is a novel human glucagon-like peptide-1 receptor (GLP-1R) agonist for the treatment of type 2 diabetes mellitus (T2DM; non-insulin dependent diabetes). The structure of lixisenatide, based on exendin-4(1-39) modified C-terminally with six Lys residues, is able to withstand physiological degradation by dipeptidyl peptidase IV. In vitro, lixisenatide bound to human GLP-1R with a greater affinity than native human GLP-1 (7-36 amide). In various in vitro and in vivo models of T2DM, lixisenatide improved glycemic measures and demonstrated promising pancreatic beta-cell-preserving actions. In patients with T2DM, subcutaneously administered lixisenatide displayed linear pharmacokinetics. In two phase II clinical trials, lixisenatide improved glucose tolerance, resulted in weight loss and lowered HbA1C, thereby causing significantly more patients to achieve target HbA1C levels compared with placebo. Lixisenatide exhibited well-established GLP-1-related gastrointestinal side effects, with mild nausea occurring most frequently; a low frequency of hypoglycemia was also reported. The results of phase III trials are awaited for confirmation of the anticipated effects of lixisenatide on glycemic measures and weight; favorable results would place lixisenatide for consideration among other GLP-1R agonists in the treatment armamentarium for T2DM.
Original languageEnglish
JournalIDrugs : the investigational drugs journal
Volume12
Issue number8
Pages (from-to)503-13
Number of pages11
Publication statusPublished - 1 Aug 2009

ID: 32266510