A review of exenatide as adjunctive therapy in patients with type 2 diabetes

摘要: Background Incretin glucagon-like peptide-1 (GLP-1) is a hormone released from cells in the gastrointestinal tract (GI), leading to glucose-dependent insulin release pancreas. It also suppresses postprandial hyperglycemia, glucagon secretion and slows gastric emptying. Exenatide (EXE), functional analog of human GLP-1, was approved by US FDA April 2005. Objective This article reviews current primary literature on clinical efficacy safety EXE treatment type 2 diabetes mellitus (DM) describes pharmacokinetics, pharmacodynamics, dosing administration EXE. Methods English-language articles were identified through search MEDLINE (1966 March 2009), International Pharmaceutical Abstracts (1970 present), Cochrane Database Systemic Reviews (1995 2009). Search terms included EXE, mellitus, emptying, glucagon, pharmacokinetics pharmacodynamics. Articles selected for review if their designs randomized, blinded controlled design that focused outcomes patients with DM. Results administered subcutaneously thigh, abdomen or upper arm within 60-minute period before morning evening meals. Its C(max) reached 2.1 hours, its T(1/2) 2.4 hours. EXE's metabolism primarily kidneys. For who received 10 microg SC BID three, 30-week, placebo-controlled studies background sulfonylureas (SUs), metformin (MET), SU + MET, there significant reductions HbA(1c) (0.77 0.86%), fasting plasma glucose (0.6 mmol/L) body weight (1.6 2.8 kg) (P 20%) reported receiving highest dose (10 vs 5 BID). Conclusions at has been proven decrease HbA(lc) 1.3% +/- 0.1% up 5.3 0.8 kg week 82. Nausea most frequently adverse event (>20%) especially being treated BID. can be safely added MET therapy, therapy combination effectively target glycemic goals Long-term, head-to-head assessing effect oral agents/insulins > = 10% are still needed fully clarify role poorly