Current understanding of the pharmacogenomics of metformin.

The identification of transporters for organic cations involved in the distribution and elimination of the antidiabetic compound metformin marks a milestone in the study of metformin's pharmacokinetics. This was followed by the urgent question of whether genetic variations in these transporters can affect efficacy and risk of adverse events associated with metformin use. After a brief historical review of the discovery of the transporters for cationic drugs, the pharmacogenetics of metformin is discussed here in the light of recent literature.