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19.05.2016 | Original Research Article | Ausgabe 11/2016 Open Access

Clinical Pharmacokinetics 11/2016

Liraglutide 3.0 mg for Weight Management: A Population Pharmacokinetic Analysis

Zeitschrift:
Clinical Pharmacokinetics > Ausgabe 11/2016
Autoren:
Rune V. Overgaard, Kristin C. Petri, Lisbeth V. Jacobsen, Christine B. Jensen
Wichtige Hinweise

Electronic supplementary material

The online version of this article (doi:10.​1007/​s40262-016-0410-7) contains supplementary material, which is available to authorized users.

Abstract

Background and Objectives

This analysis used a population pharmacokinetic approach to identify covariates that influence plasma exposure of liraglutide 3.0 mg, a glucagon-like peptide-1 (GLP-1) receptor agonist approved for weight management in overweight and obese individuals.

Methods

Samples for pharmacokinetic analysis were drawn at weeks 2, 12 and 28 of the phase IIIa SCALE Obesity and Prediabetes (N = 2339) and SCALE Diabetes (N = 584) trials. Dose proportionality of liraglutide in obese subjects was investigated using data from a phase II dose-finding study (N = 331).

Results

Dose-proportional exposure of liraglutide up to and including 3.0 mg was confirmed. Body weight and sex influenced exposure of liraglutide 3.0 mg, while age ≥70 years, race, ethnicity and baseline glycaemic status did not. Compared with a reference subject weighing 100 kg, exposure of liraglutide 3.0 mg was 44 % lower for a subject weighing 234 kg (90 % CI 41–47), 41 % higher for a subject weighing 60 kg (90 % CI 37–46), and 32 % higher (90 % CI 28–35) in females than males with the same body weight. Neither injection site nor renal function significantly influenced exposure of liraglutide 3.0 mg (post hoc analysis).

Conclusion

Population pharmacokinetics of liraglutide up to and including 3.0 mg daily in overweight and obese adults demonstrated dose-proportional exposure, and limited effect of covariates other than sex and body weight. These findings were similar to those previously observed with liraglutide up to 1.8 mg in subjects with type 2 diabetes mellitus. Further analysis of exposure–response relationship and its effect on dose requirements is addressed in a separate publication.

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Zusatzmaterial
Supplementary material 1 (PDF 620 kb)
40262_2016_410_MOESM1_ESM.pdf
Literatur
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