Pharmacokinetic and pharmacodynamic properties of taspoglutide, a once-weekly, human GLP-1 analogue, after single-dose administration in patients with Type 2 diabetes.
OBJECTIVE
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.
Kapitza
C
C
Profil Institut für Stoffwechselforschung GmbH, Neuss, Germany.
Heise
T
T
Birman
P
P
Jallet
K
K
Ramis
J
J
Balena
R
R
D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D005260:Female; D052216:Glucagon-Like Peptide 1 / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D007279:Injections, Subcutaneous; D008297:Male; D008875:Middle Aged; D010455:Peptides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016896:Treatment Outcome
D003692:Delayed-Action Preparations; D007004:Hypoglycemic Agents; D010455:Peptides; C541736:taspoglutide; D052216:Glucagon-Like Peptide 1