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BioDrugs. 2015 Dec;29(6):407-18. doi: 10.1007/s40259-015-0143-4.
Dulaglutide (Trulicity™) is a once-weekly subcutaneously administered glucagon-like peptide-1 (GLP-1) receptor agonist produced by recombinant DNA technology and approved in numerous countries as an adjunct to diet and exercise for the treatment of adults with type 2 diabetes (T2DM). In randomized controlled trials in patients with T2DM, dulaglutide monotherapy was noninferior to once-daily subcutaneous liraglutide monotherapy and significantly more effective than oral metformin monotherapy in improving glycemic control at 26 weeks. When used in combination with other agents (including metformin, metformin and a sulfonylurea, metformin and oral pioglitazone, and prandial insulin ± metformin), dulaglutide was noninferior to once-daily liraglutide and significantly more effective than once-daily oral sitagliptin, twice-daily subcutaneous exenatide, and once-daily subcutaneous insulin glargine in terms of improvements in glycated hemoglobin from baseline at 26 or 52 weeks, in trials of 26-104 weeks' duration. Moreover, dulaglutide 1.5 mg once weekly, but not 0.75 mg once weekly, was associated with consistent reductions form baseline in bodyweight. Improvements in glycemic control and bodyweight were maintained during long-term treatment (up to 2 years). Dulaglutide was generally well tolerated, with a low inherent risk of hypoglycemia. The most frequently reported adverse events in clinical trials were gastrointestinal-related (e.g., nausea, vomiting, and diarrhea). Thus, dulaglutide is a useful option for the treatment of adult patients with T2DM.
度拉糖肽(Trulicity™)是一种每周一次皮下注射的胰高血糖素样肽-1(GLP-1)受体激动剂,采用重组 DNA 技术生产,已在多个国家获得批准,与饮食和运动联合用于治疗 2 型糖尿病(T2DM)成人患者。在 T2DM 患者的随机对照试验中,度拉糖肽单药治疗与每日一次皮下注射利拉鲁肽单药治疗非劣效,在 26 周时改善血糖控制的疗效明显优于每日一次口服二甲双胍单药治疗。当与其他药物联合使用(包括二甲双胍、二甲双胍和磺脲类药物、二甲双胍和口服吡格列酮、以及餐时胰岛素+二甲双胍)时,度拉糖肽在 26 或 52 周时与每日一次利拉鲁肽相比非劣效,在 26-104 周的试验中,与每日一次口服西格列汀、每日两次皮下注射艾塞那肽和每日一次皮下注射甘精胰岛素相比,改善糖化血红蛋白从基线的疗效更优。此外,每周一次 1.5mg 度拉糖肽,但不是每周一次 0.75mg 度拉糖肽,与体重从基线的持续降低相关。在长期治疗(长达 2 年)期间,血糖控制和体重的改善得以维持。度拉糖肽总体上耐受性良好,低血糖的固有风险低。临床试验中报告的最常见不良事件是胃肠道相关的(如恶心、呕吐和腹泻)。因此,度拉糖肽是治疗 T2DM 成年患者的一种有用选择。