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Clin Pharmacol Ther. 2008 Nov;84(5):559-62. doi: 10.1038/clpt.2008.61. Epub 2008 Apr 9.

Genetic variants of the organic cation transporter 2 influence the disposition of metformin.

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Department of Pharmacology and Pharmacogenomics Research Center, Inje University College of Medicine, Busan, Korea.


Genetic variants of the organic cation transporter 2 (protein, OCT2; gene, SLC22A2) were evaluated for their contribution to the variations in the pharmacokinetics of metformin, especially to its renal elimination. Genetic variants of SLC22A2 (c.596C>T, c.602C>T, and c.808G>T) showed significant differences in metformin pharmacokinetics when compared with the reference genotype, with higher peak plasma concentration (C(max)) and area under the curve (AUC) and lower renal clearance (Cl(renal)), thereby suggesting that a decrease in transport function associated with the SLC22A2 variants results in reduced Cl(renal) of metformin and consequently leads to increased plasma concentrations.

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