Liraglutide: from clinical trials to clinical practice
Liraglutide: from clinical trials to clinical practice
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DOI：
10.1111/j.1463-1326.2012.01576.x
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发表时间：
2012-04-01
影响因子：
5.8
通讯作者：
Gough, S. C. L.
中科院分区：
文献类型：
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作者：
Gough, S. C. L.
利拉鲁肽（Liraglutide）是一种每日一次的胰高血糖素样肽-1受体激动剂，已被批准在美国和日本（但未在欧洲或加拿大）作为单药治疗，并与选定的口服药物联合（所有地区）用于治疗2型糖尿病患者。当地咨询机构正在就利拉鲁肽在治疗途径中最合适的位置提出指导意见。从其3期临床试验计划中可以明显看出，利拉鲁肽与其他早期使用的抗糖尿病药物（如格列美脲和西格列汀）相比，提供了更好的血糖控制。主要的额外益处包括低血糖发生率低和临床相关的体重减轻，尽管这些益处可能通过同时使用磺脲（SU）治疗而得到改善，并且在低血糖的情况下，可能需要减少SU剂量。总的来说，利拉鲁肽的特点是相似的，在某些方面优于每日两次的艾塞那肽。利拉鲁肽治疗的实施是直接的，1周后从开始剂量0.6到1.2 mg/天的简单剂量滴定；一些患者可能受益于额外的滴定至1.8 mg/天。治疗方法为皮下注射。这与在治疗途径早期使用的其他药物形成对比，但临床数据表明，尽管给药方法不同，利拉鲁肽的患者总体治疗满意度与西格列汀相似（1.2 mg）或更好（1.8 mg）。一些患者在开始利拉鲁肽治疗时可能会感到恶心，但滴定方案旨在提高耐受性，临床数据表明恶心是短暂的。
Liraglutide, a once-daily glucagon-like peptide-1 receptor agonist, is approved for use as monotherapy in the USA and Japan (but not in Europe or Canada) and in combination with selected oral agents (all regions) for the treatment of patients with type 2 diabetes. Guidance from local advisory bodies is emerging on the most appropriate place for liraglutide in the treatment pathway. It is apparent from its phase 3 clinical trial programme that liraglutide provides superior glycaemic control compared with that achieved with other antidiabetic agents used early in the treatment pathway (e.g. glimepiride and sitagliptin). Key additional benefits include a low incidence of hypoglycaemia and clinically relevant weight loss, although these benefits may be ameliorated by concomitant sulphonylurea (SU) treatment and, in the case of hypoglycaemia, reduction of the SU dose may be necessary. Overall, the profile of liraglutide is similar and, in some aspects, superior to twice-daily exenatide. The implementation of liraglutide therapy is straightforward, with simple dose titration from the starting dose of 0.6 to 1.2 mg/day after 1 week; some patients may benefit from additional titration to 1.8 mg/day. Treatment is self-administered by subcutaneous injection. This contrasts with other agents used early in the treatment pathway, but clinical data suggest patients' overall treatment satisfaction with liraglutide is similar (1.2 mg) or better (1.8 mg) than that with sitagliptin despite differing administration methods. Some patients may experience nausea when initiating liraglutide treatment, but the titration regimen is designed to improve tolerability and clinical data indicate nausea is transient.