Cetero Research, San Antonio, TX, USA.
Diabetes Obes Metab. 2011 Nov;13(11):982-9. doi: 10.1111/j.1463-1326.2011.01428.x.
To compare exenatide and sitagliptin glucose and glucoregulatory measures in subjects with type 2 diabetes.
An 8-week, double-blind, randomized, crossover, single-centre study. Eighty-six subjects (58% female, body mass index 35 ± 5 kg/m², haemoglobin A1c 8.3 ± 1.0%) received either exenatide 10 µg (subcutaneous) twice daily or sitagliptin 100 mg (oral) daily for 4 weeks and crossed to the other therapy for an additional 4 weeks. Main outcome was time-averaged glucose during the 24-h inpatient visits.
Both treatments decreased average 24-h glucose, but exenatide had a greater effect [between-group difference: -0.67 mmol/l, 95% confidence interval (CI): -0.9 to -0.4 mmol/l]. Both treatments decreased 2-h postprandial glucose (PPG), area under the curve of glucose above 7.8 mmol/l (140 mg/dl) and 11 mmol/l (200 mg/dl) and increased the time spent with glucose between 3.9 and 7.8 mmol/l (70 and 140 mg/dl) during 24 h, but exenatide had a significantly greater effect (p < 0.05). Both treatments decreased postprandial serum glucagon, with exenatide having a greater effect (p < 0.005). Both treatments decreased fasting blood glucose to a similar degree (p = 0.766). Sitagliptin increased, while exenatide decreased, postprandial intact glucagon-like peptide-1. Both drugs improved homeostasis model assessment of β-cell function (HOMA-B), with exenatide having a significantly greater effect (p = 0.005). Both exenatide and sitagliptin decreased 24-h caloric intake, with exenatide having a greater effect (p < 0.001). There was no episode of major hypoglycaemia. Adverse events were mild to moderate and mostly gastrointestinal in nature with exenatide. No study withdrawals were due to an adverse event.
Compared to sitagliptin, exenatide showed significantly lower average 24-h glucose, 2-h PPG, glucagon, caloric intake and improved HOMA-B.
比较艾塞那肽和西格列汀在 2 型糖尿病患者中的血糖和糖调节指标。
一项 8 周、双盲、随机、交叉、单中心研究。86 例受试者（58%为女性，体重指数 35 ± 5 kg/m²，糖化血红蛋白 8.3 ± 1.0%）分别接受艾塞那肽 10 µg（皮下注射）每日 2 次或西格列汀 100 mg（口服）每日 1 次治疗 4 周，然后交叉至另一治疗方案再治疗 4 周。主要结局是 24 小时住院期间的平均血糖。
两种治疗均降低了平均 24 小时血糖，但艾塞那肽的效果更大[组间差异：-0.67 mmol/l，95%置信区间（CI）：-0.9 至 -0.4 mmol/l]。两种治疗均降低了餐后 2 小时血糖（PPG）、血糖曲线下面积（AUC）超过 7.8 mmol/l（140 mg/dl）和 11 mmol/l（200 mg/dl），并增加了 24 小时内血糖在 3.9 至 7.8 mmol/l（70 至 140 mg/dl）之间的时间，但艾塞那肽的效果显著更大（p < 0.05）。两种治疗均降低了餐后血清胰高血糖素，艾塞那肽的效果更大（p < 0.005）。两种治疗均使空腹血糖降低至相似程度（p = 0.766）。西格列汀增加，而艾塞那肽降低了餐后完整胰高血糖素样肽-1。两种药物均改善了β细胞功能的稳态模型评估（HOMA-B），艾塞那肽的效果显著更大（p = 0.005）。艾塞那肽和西格列汀均降低了 24 小时热量摄入，艾塞那肽的效果更大（p < 0.001）。无重大低血糖发作。不良事件轻微至中度，以胃肠道为主，艾塞那肽的不良事件更多。无因不良事件而退出研究的情况。
与西格列汀相比，艾塞那肽显示出明显更低的平均 24 小时血糖、2 小时 PPG、胰高血糖素、热量摄入和改善的 HOMA-B。
