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

Abstract

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.

• Authors: C Kapitza, T Heise, P Birman, K Jallet, J Ramis, R Balena
• Journal: Diabetic medicine : a journal of the British Diabetic Association (Diabet Med) Vol. 26 Issue 11 Pg. 1156-64 (Nov 2009) ISSN: 1464-5491 [Electronic] England
• PMID: 19929995 (Publication Type: Clinical Trial, Phase I, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)

Chemical References

• Delayed-Action Preparations
• Hypoglycemic Agents
• Peptides
• taspoglutide
• Glucagon-Like Peptide 1

Topics

• Delayed-Action Preparations (administration & dosage, pharmacokinetics)
• Diabetes Mellitus, Type 2 (drug therapy)
• Dose-Response Relationship, Drug
• Double-Blind Method
• Drug Administration Schedule
• Female
• Glucagon-Like Peptide 1 (administration & dosage, pharmacokinetics)
• Humans
• Hypoglycemic Agents (administration & dosage, pharmacokinetics)
• Injections, Subcutaneous
• Male
• Middle Aged
• Peptides (administration & dosage, pharmacokinetics)
• Treatment Outcome