ABSTRACT
Drug transporters play vital roles in absorption, distribution and excretion of drugs. Understanding the transport activity can improve the effectiveness and safety of drugs and guide clinical rational use of drugs. Metformin is a first-line drug in the treatment of type 2 diabetes mellitus, of which the pharmacokinetics involves several transporters. The changes in expression and function of these transporters affect directly the pharmacokinetics/pharmacodynamics of metformin. This paper reviews the research progress of pharmacokinetics of metformin based on transporters, and these transporters are organic cation transporters (OCTs), multidrug and toxin extrusion proteins (MATE), plasma membrane monoamine transporter protein (PMAT), serotonin reuptake transporter (SERT), thiamine transporter 2 (THTR-2), and carnitine/organic cation 1 (OCTN1).