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Transporter Drug Interactions

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The ADME Encyclopedia

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Definition

Drug transporters are membrane-bound cellular proteins that act as gatekeepers to facilitate either (1) the entry or (2) the exit of endobiotics or xenobiotics (drugs), into or out of cells, respectively. Two superfamilies exist, the ATP-binding cassette (ABC) transporter family, which is responsible for efflux out of cells, and the solute carrier (SLC) transporter family that primarily uptake into cells. Together these transporters can influence the intracellular concentrations of drugs within tissues which, in turn, can impact both their efficacy and toxicity. Furthermore, due to their expression on enterocytes of the gastrointestinal tract, on hepatocytes, at the blood-brain barrier, and on renal proximal tubule cells, transporters can determine pharmacokinetics by modulating the absorption, distribution, metabolism, and elimination (ADME) of drugs that are substrates.

Mechanistic changes in these ADME processes, and subsequently in the pharmacokinetic profile of a...

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Author information

Authors and Affiliations

  1. Department of ADME Sciences, Cyprotex Discovery Ltd (an Evotec company), Cheshire, UK

    Robert Elsby

  2. Cyprotex Discovery Ltd (an Evotec company), Cheshire, UK

    Philip Butler & Robert J. Riley

Authors
  1. Robert Elsby
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  2. Philip Butler
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  3. Robert J. Riley
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Corresponding author

Correspondence to Philip Butler .

Editor information

Editors and Affiliations

  1. University of La Plata (UNLP), Argentinian National Council of Scientific and Technical Research (CONICET), La Plata, Argentina

    Alan Talevi

Section Editor information

  1. Medicinal Chemistry, Department of Biological Sciences, Faculty of Exact Sciences, National University of la Plata (UNLP) - Argentinean National Council of Scientific and Technical Research (CONICET), La Plata, Buenos Aires, Argentina

    Alan Talevi

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Elsby, R., Butler, P., Riley, R.J. (2022). Transporter Drug Interactions. In: Talevi, A. (eds) The ADME Encyclopedia. Springer, Cham. https://doi.org/10.1007/978-3-030-84860-6_90

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