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百达扬:首款每周一次的胰高血糖素样肽-1(GLP-1)受体激动剂(艾塞那肽长效注射剂)

[Bydureon: first once weekly GLP-1 receptor agonist (exenatide LAR)].

作者信息

Scheen A J

出版信息

Rev Med Liege. 2014 Apr;69(4):214-9.

Abstract

Bydureon is a new galenic formulation (long-acting release) of exenatide, the first agonist of Glucagon-Like Peptide-1 (GLP-1) receptors having been commercialized for the management of type 2 diabetes. The microsphere technology permits a prolonged absorption of exenatide from the subcutaneous depot, which allows one injection per week instead of two injections per day with the initial formulation of exenatide (Byetta). The clinical development programme DURATION showed that exenatide 2 mg once weekly more markedly reduces glycated haemoglobin (HbA(1c)), with a similar weight loss but a better digestive tolerance profile (less nausea and vomiting after treatment initiation), compared with the twice daily 10 microg exenatide. When compared to other glucose-lowering agents, once weekly exenatide is more efficacious than sitagliptin, pioglitazone or basal insulin (glargine or detemir), with the advantage of producing weight loss and lowering arterial blood pressure. It does not induce hypoglycaemia and does not necessarily require home blood glucose monitoring, two advantages compared with insulin therapy. Bydureon is currently only reimbursed in Belgium after failure of and in addition to metformin-sulfonylurea combination.

摘要

百达扬是艾塞那肽的一种新剂型(长效释放),它是首个用于治疗2型糖尿病的已商业化的胰高血糖素样肽-1(GLP-1)受体激动剂。微球技术使艾塞那肽能从皮下储库中持续吸收,这使得每周只需注射一次,而不像艾塞那肽的初始剂型(百泌达)那样每天注射两次。“DURATION”临床研发项目表明,与每日两次注射10微克艾塞那肽相比,每周一次注射2毫克艾塞那肽能更显著地降低糖化血红蛋白(HbA1c),减重效果相似,但消化耐受性更好(治疗开始后恶心和呕吐较少)。与其他降糖药物相比,每周一次注射艾塞那肽比西格列汀、吡格列酮或基础胰岛素(甘精胰岛素或地特胰岛素)更有效,具有减重和降低动脉血压的优势。它不会诱发低血糖,也不一定需要家庭血糖监测,这两点相对于胰岛素治疗来说是优势。目前,在比利时,只有在二甲双胍-磺脲类药物联合治疗失败后且作为附加治疗时,百达扬才予以报销。

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