Membrane Transporters in Drug Development: Recent Advances

Dear Colleagues,

Membrane transporters have a key role in drug metabolism and toxicity; therefore the process of current drug development has to be concerned with the proper and early exploration of these potential interactions. In this regard the most important transporters are the ABC drug extrusion pumps, especially the promiscuous multidrug transporters, and the various SLC transporters, promoting the uptake of a large number of drugs, as well as endo-and xenobiotics. 

The direct involvement of these transporters in the absorption, distribution, metabolism, excretion, and toxicity (ADME-tox) of the pharmacological agents prompted the major regulatory agencies, including FDA and EMA, to make the preclinical screening of such interactions obligatory. Interestingly, numerous drugs, not directly transported by these membrane proteins, still strongly inhibit specific transporter pathways thus, through drug-drug interactions, indirectly modify ADME-tox parameters. 

In addition to their effects on general drug metabolism, membrane transporters may strongly increase (SLC transporters) or reduce (ABC efflux pumps) the intracellular availability of anticancer drugs, as well as the penetration of pharmacological agents through important tissue barriers, such as the blood-brain or blood-placenta barriers. Potential drug-induced organ damages, e.g. DILI (drug-induced liver injury) are also important aspects of transporter-drug interactions. 

The aim of this Special Issue is to offer comprehensive reviews to our readers on the recent advances in the area of transporter-drug interactions, also calling attention to the increasing importance and regulatory requirements on examining such interactions in the early, as well is in the following phases of drug development.

Prof. Dr. Balázs Sarkadi
Guest Editor

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• transporters affecting drug ADME-tox
• ABC drug transporters
• SLC drug transporters
• transporters in anticancer drug development
• transporters in drug-drug interactions
• regulatory issues in transporter-drug interactions
• transporters in drug-induced organ damage.