Steady-state Pharmacokinetics of Metformin is Independent of the OCT1 Genotype in Healthy Volunteers

Overview

Journal Eur J Clin Pharmacol

Specialty Pharmacology

Date 2015 May 6

PMID 25939711

Citations 27

Authors

Mette Marie Hougaard Christensen

Kurt Hojlund

Ole Hother-Nielsen

Tore Bjerregaard Stage

Per Damkier

Henning Beck-Nielsen

Kim Brosen

Affiliations

Soon will be listed here.

Abstract

Purpose: The aim of the study was to determine the steady-state pharmacokinetics of metformin in healthy volunteers with different numbers of reduced-function alleles in the organic cation transporter 1 gene (OCT1).

Methods: The study was conducted as part of a randomized cross-over trial. Thirty-four healthy volunteers with known OCT1 genotypes (12 with two wild-type alleles, 13 with one and 9 with two reduced-function alleles) were included. In one of the study periods, they were titrated to steady-state with 1 g metformin twice daily.

Results: Neither AUC(0-12), C(max) nor Cl(renal) were statistically significantly affected by the number of reduced-function alleles (0, 1 or 2) in OCT1: (AUC(0-12): 0, 1, 2: 14, 13 and 14 h ng/L (P = 0.61)); (C(max): 0, 1, 2: 2192, 1934 and 2233 ng/mL, (P = 0.26)) and (Cl(renal): 0, 1, 2: 31, 28 and 30 L/h (P = 0.57)) CONCLUSIONS: In a cohort of healthy volunteers, we found no impact of different OCT1 genotypes on metformin steady-state pharmacokinetics.

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