Disease-Associated Changes in Drug Transporters May Impact the Pharmacokinetics and/or Toxicity of Drugs: A White Paper From the International Transporter Consortium

Clin Pharmacol Ther. 2018 Nov;104(5):900-915. doi: 10.1002/cpt.1115. Epub 2018 Jul 12.


Drug transporters are critically important for the absorption, distribution, metabolism, and excretion (ADME) of many drugs and endogenous compounds. Therefore, disruption of these pathways by inhibition, induction, genetic polymorphisms, or disease can have profound effects on overall physiology, drug pharmacokinetics, drug efficacy, and toxicity. This white paper provides a review of changes in transporter function associated with acute and chronic disease states, describes regulatory pathways affecting transporter expression, and identifies opportunities to advance the field.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease*
  • Animals
  • Chronic Disease / drug therapy*
  • Drug Interactions
  • Drug-Related Side Effects and Adverse Reactions / etiology
  • Drug-Related Side Effects and Adverse Reactions / metabolism
  • Humans
  • Membrane Transport Modulators / metabolism
  • Membrane Transport Modulators / pharmacology*
  • Membrane Transport Proteins / drug effects*
  • Membrane Transport Proteins / genetics
  • Membrane Transport Proteins / metabolism*
  • Models, Biological
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics*
  • Risk Assessment


  • Membrane Transport Modulators
  • Membrane Transport Proteins
  • Pharmaceutical Preparations