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    演示文稿1 演示文稿1 Presentation Transcript

    • Liraglutide for Type 2 Diabetes Mellitus Wang Hongchen Xue Zhijuan Yan Zhuopeng
    • Contents 1 Introduction 2 Liraglutide – Victoza® 3 Clinical data 4 Conclusion
    • WHO defined diabetes mellitus as “a state ofabsolute or relative insulin deficiency,characterized by hyperglycemia and the risk ofmicrovascular and macrovascular complications.”
    • Types of DiabetesThere are three main types of diabetes:Type 1 diabetes: results from the bodys failure to produce insulin, and presently requires the person to inject insulin.Type 2 diabetes: results from insulin resistance, a condition in which cells fail to use insulin properly, sometimes combined with an absolute insulin deficiency.Gestational diabetes: is when pregnant women, who have never had diabetes before, have a high blood glucose level during pregnancy.
    • Classical Symptoms • Polyuria • Polydipsia • Polyphagia
    • Insulin &SynthesisFauci AS, Kasper DL, Braunwald E, Hauser SL, Longo DL, Jameson JL, Loscalzo J: Harrison’s Principles of Internal Medicine, 17th Edition: http://www.accessmedicine.com
    • Insulin Receptor and Drugs· The insulin receptor is a transmembrane receptor that is activated by insulin.· The main activity of activation of the insulin receptor is inducing glucose uptake.Metformin, sulfonylureas, nonsulfonylurea secretagogues,alpha glucosidase inhibitors, and thiazolidinediones.
    • common medicines SUs Metformin t1/2: 5h t1/2: 6.2h Side-effect: Hypoglycemia Side-effect: GI system Weight gain Lactic acidosis Metallic taste Acarbose TZDs t1/2: 2h t1/2: 3-7hSide-effect: Hypoglycemia Side-effect: GI symptoms
    • Incretin-base therapy
    • Liraglutide
    • Victoza®· Helps lower A1C level and lower blood sugar· Helps keep beta cells in pancreas working· Helps lose weight· Easy to use NovoTwist® NovoFine®
    • In Vitro Assays• Liraglutide was tested for its receptor selectivity in binding and functional assays comprising more than 75 different receptors, ion-channels and drug transporters.• Enhancement of glucose-dependent insulin secretion• Sulfonylureas uncouple the glucose-dependency of GLP-1 induced insulin secretion.
    • In Vivo Assays• Liraglutide is a potent agonist on cloned GLP-1 receptors from human as well as mouse, rat, rabbit, pig and monkey.• Liraglutide treatment of all animal models of diabetes was characterized by a consistent, acute, and dose-dependent reduction in plasma glucose.
    • Clinical Data• The efficacy and safety of liraglutide were assessed in five double-blind, randomized, controlled clinical trials involving a total of 3,978 patients with type 2 diabetes.• PhaseⅠ: Liraglutide is reported to produce weight loss and reduce food intake.• Phase Ⅱ: The program was supported by evidence from five phase Ⅱ trials.• Phase Ⅲ: A population pharmacokinetic analysis from the long-term phase 3 Trial 1573 (52-week monotherapy trial).
    • Outline of Treatment of the FiveLong-term Phase 3 Trials
    • Conclusion• Diabetes Mellitus is a disease of hyperglycemia• Liraglutide: high effciency, low risk drug• Diet, regular exercises, proper eating habits can reduce diabetes
    • Thank You!
    • References