Profil Institut für Stoffwechselforschung GmbH, Neuss, Germany.
Diabet Med. 2009 Nov;26(11):1156-64. doi: 10.1111/j.1464-5491.2009.02854.x.
The study objectives were to evaluate the pharmacokinetic and pharmacodynamic properties, as well as safety and tolerability, of single doses of taspoglutide, a human glucagon-like peptide-1 (GLP-1) analogue.
In a double-blind, placebo-controlled study, 48 patients with Type 2 diabetes [mean age 56 +/- 7 years; mean body mass index (BMI) 30.4 +/- 3.0 kg/m(2)] inadequately controlled with metformin (< or = 2 g/day) were enrolled in three sequential cohorts; 12 patients in each cohort were randomized to a single subcutaneous injection of taspoglutide (1, 8 or 30 mg) and four received placebo.
Plasma concentrations peaked within 24 h after injection and were sustained for > or = 14 days with all doses. In comparison with placebo, the 8- and 30-mg doses of taspoglutide significantly reduced glycaemic parameters, including 24-h blood glucose and 5-h postprandial glucose areas under the curve (AUCs), for up to 14 days with the 30-mg dose (P < 0.001). The most common adverse events, primarily gastrointestinal in nature, were dose-dependent and transient.
A single dose of taspoglutide significantly improved glycaemic parameters in Type 2 diabetes patients for up to 14 days. The formulation was well tolerated and appears suitable for weekly administration.
本研究旨在评估单剂量塔斯格鲁肽（一种人胰高血糖素样肽-1（GLP-1）类似物）的药代动力学和药效学特性，以及安全性和耐受性。
在一项双盲、安慰剂对照研究中，48 例 2 型糖尿病患者（平均年龄 56±7 岁；平均体重指数（BMI）30.4±3.0kg/m2），他们正在接受二甲双胍（<或=2g/天）治疗，但血糖控制不佳，这些患者被分为三个连续队列；每个队列中有 12 例患者被随机分配接受单次皮下注射塔斯格鲁肽（1、8 或 30mg），另有 4 例接受安慰剂。
注射后 24 小时内血浆浓度达到峰值，所有剂量的药物在>或=14 天内持续维持。与安慰剂相比，8mg 和 30mg 剂量的塔斯格鲁肽可显著降低血糖参数，包括 24 小时血糖和 5 小时餐后血糖曲线下面积（AUC），在 30mg 剂量下可维持 14 天（P<0.001）。最常见的不良反应主要为胃肠道性质，与剂量相关且为一过性。
单次给予塔斯格鲁肽可显著改善 2 型糖尿病患者的血糖参数，最长可达 14 天。该制剂具有良好的耐受性，每周给药一次可能是可行的。
