Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics.

作者: Y Shu , C Brown , RA Castro , RJ Shi , ET Lin

DOI: 10.1038/SJ.CLPT.6100275

关键词:

摘要: The goal of this study was to determine the effects genetic variation in organic cation transporter 1, OCT1, on pharmacokinetics antidiabetic drug, metformin. Twenty healthy volunteers with known OCT1 genotype agreed participate study. Each subject received two oral doses metformin followed by collection blood and urine samples. genotypes had a significant (P<0.05) effect pharmacokinetics, higher area under plasma concentration-time curve (AUC), maximal concentration (Cmax), lower volume distribution (V/F) individuals carrying reduced function allele (R61C, G401S, 420del, or G465R). mice less than humans possibly reflecting species differences hepatic expression level transporter. Our studies suggest that is determinant pharmacokinetics.

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