EMA Guidance on transporters (Click to view)

Transporters have become increasingly important in drug development due to the major role they play in absorption, distribution and excretion of endogenous and exogenous compounds, as transporter-mediated drug-drug interactions (DDI) are associated with potential toxicological and pharmacological consequences. As shown in numerous publications, the effects of transporters on the pharmacokinetics of several drugs and associated DDI have been reported. Consequently, recent guidance documents released by the US FDA and European Medicines Agency (EMA) emphasize the importance of evaluating the potential of new drug candidates for transporter-mediated DDI.

Solute carrier (SLC) transporters are located in the small intestine, liver, kidney, blood-brain barrier, and so on. They play a role in the up-take of various drugs, as well as endogenous nutrients into cells and thus may influence the ADME properties of, or indeed adverse reactions to, a compound of interest. Thus, investigation of SLC transporters is expected to be helpful during drug development.