ABSTRACT
Most mammalian cell membranes contain various transporter systems, which are effective in taking up a great number of endogenous and exogenous molecules that the cells need, or in extruding endogenous and exogenous molecules that the cells want to get rid of. In humans, some of these transporters also play a significant role in the processes of drug absorption, distribution, metabolism, and excretion of drugs. Perhaps the most compelling clinical evidence of a transporter-mediated drug interaction is obtained from drugs that are eliminated predominately by drug transporters. A major challenge in the therapeutic treatment of cancer is the so-called multidrug resistance to anticancer drugs. In addition to transporter inhibition, drug interactions caused by transporter induction have also been reported. An important question that is often asked is how significant the transporter- mediated drug interactions would likely be in clinical settings.
