Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1.

Article Details

Citation

Copy to clipboard

Kimura N, Masuda S, Tanihara Y, Ueo H, Okuda M, Katsura T, Inui K

Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1.

Drug Metab Pharmacokinet. 2005 Oct;20(5):379-86.

PubMed ID

16272756 [ View in PubMed

]

Abstract

Although metformin, a cationic agent for type II diabetes, shows its pharmacological effect in the liver, the drug is mainly eliminated into urine. The tissue selectivity based on the function of drug transporters is unclear. In the present study, the transport of metformin was examined using HEK293 cells transiently transfected with five human renal organic ion transporter cDNAs. Human OCT1 and OCT2, but not OAT1, OAT3 or OCT2-A, stimulated the uptake. A kinetic analysis of metformin transport demonstrated that the amount of plasmid cDNA for transfection was also important parameter to the quantitative elucidation of functional characteristics of transporters, and both human and rat OCT2 had about a 10- and 100-fold greater capacity to transport metformin than did OCT1, respectively. In male rats, the mRNA expression level of rOCT2 in the whole kidneys was 8-fold greater than that of rOCT1 in the whole liver. The in vivo distribution of metformin in rats revealed that the expression level of renal OCT2 was a key factor in the control of the concentrative accumulation of metformin in the kidney. These findings suggest that metformin is a superior substrate for renal OCT2 rather than hepatic OCT1, and renal OCT2 plays a dominant role for metformin pharmacokinetics.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Metformin	Solute carrier family 22 member 2	Protein	Humans	Unknown	Substrate Inhibitor	Details

Polypeptides

Name	UniProt ID
Solute carrier family 22 member 2	O15244	Details
Solute carrier family 22 member 1	O15245	Details

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
Integrate drug-drug interactions in your software
Dalfampridine Metformin	The serum concentration of Dalfampridine can be increased when it is combined with Metformin.
Metformin Lamotrigine	The serum concentration of Metformin can be increased when it is combined with Lamotrigine.

Identify potential medication risks

Easily compare up to 40 drugs with our drug interaction checker.

Get severity rating, description, and management advice.

Learn more