Pharmacokinetic and pharmacodynamic properties of taspoglutide, a once‐weekly, human GLP‐1 analogue, after single‐dose administration in patients with Type 2 diabetes

AIMS: 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. METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.