Clinical studies of exenatide once weekly, a novel, once weekly GLP-1 receptor agonist for improved management of type 2 diabetes [Klinische Studien zu Exenatide 1 × wöchentlich - Ein neuer, einmal wöchentlicher GLP-1-Rezeptoragonist zur Verbesserung der Therapie des Typ-2-Diabetes]
Gallwitz B.,Medizinische Klinik IV |
Schnell O.,Forschergruppe Diabetes Am Helmholz Zentrum |
Forst T.,Institute For Klinische Forschung Und Entwicklung Ikfe |
Bachmann O.,Lilly Deutschland GmbH |
Haupt A.,Lilly Deutschland GmbH
Diabetologie und Stoffwechsel | Year: 2010
Exenatide once weekly (exenatide QW) is a new dosage form of the active drug exenatide. Exenatide QW's microsphere technology enables very slow release due to the use of a slowly biodegradable polymer as the exenatide carrier. This changes both the effect and adverse effect profiles versus the short-acting receptor stimulation produced by exenatide two times daily. Long-term stimulation of GLP-1 receptors results in superior lowering of fasting blood glucose levels and HbA In subjects on first-line treatment with metformin, exenatide QW produced superior HbAreduction, with mean HbAreductions of 1.5-1.9 % versus exenatide two times daily (HbA- 1.0 %), sitagliptin (HbA- 0.9 %), pioglitazone (HbA- 1.2 %) and insulin glargine (HbA- 1.3 %). Because of the less pronounced inhibition of gastric emptying, postprandial glycemia reduction is somewhat less effective than with conventional exenatide. Against that, gastrointestinal toxicity is reduced by about one-third (20 % versus 35 %). In addition, a relevant loss in mean weight (ranging from 2.3 to 3.7 kg) was seen in all studies. Benefits were also documented for blood pressure, lipid profiles and other cardiovascular risk factors. A cardiovascular outcome study has been launched which is expected to generate data within the next few years. Clinical study data available to date show that exenatide QW is a useful therapeutic option in subjects with poorly controlled type 2 diabetes on metformin, even though the value of exenatide QW has not yet been proven in real-life clinical practice and in long-term studies. © Georg Thieme Verlag KG Stuttgart - New York.