Exenatide extended release

Abstract

Exenatide once weekly (ExeOW,Bydureon Astra Zeneca), a drug belonging to the class of glucagon-like peptide-1 (GLP-1)receptor agonists, is the first agent approved for treatment of type 2 diabetes that can be administered on a weekly basis. Exenatide once-weekly is under development as monotherapy as an adjunct to diet and exercise or as a combination therapy with an oral antidiabetes drug in adults with type 2 diabetes. This long-acting formulation contains the active ingredient of the original exenatide twice-daily formulation encapsulated in 0.06-mm-diameter microspheres After mechanical suspension and subcutaneous injection by the patient.A small amount of loosely bound surface exenatide, typically less than 1%,releases in the first few hours, whereas drug located in deeper interstices diffuses out more slowly (time to maximum,2 d and glycolic acid,which are subsequently eliminated as carbon dioxide and water. For EQW, plasma exeweeks).Fully encapsulated exenatide (i.e, drug initially inaccessible to diffusion) releases over a still longer period (time to maximum 7 weeks) as the PLG matrix hydrolyzes into lactic acinatide concentrations reach the therapeutic range by 2 weeks and steady state by 6–7 weeks.In comparative trials, EQW improved hemoglobin A1c more than EBID, sitagliptin, pioglitazone, or insulin glargine and reduced fasting plasma glucose more than EBID. EQW is the first glucose-lowering agent that is administered once weekly.