In vitro methods to support transporter evaluation in drug discovery and development

Clin Pharmacol Ther. 2013 Jul;94(1):95-112. doi: 10.1038/clpt.2013.81. Epub 2013 Apr 10.


This white paper addresses current approaches and knowledge gaps concerning methods to assess the role of transport proteins in drug/metabolite disposition in humans. The discussion focuses on in vitro tools to address key questions in drug development, including vesicle- and cell-based systems. How these methods can be used to assess the liability of compounds for transporter-based drug-drug interactions (DDIs) in vivo is also explored. Existing challenges and approaches to examine the involvement of transporters in drug disposition are discussed.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Biological Transport / drug effects*
  • Drug Discovery / methods*
  • Drug Evaluation, Preclinical / methods
  • Drug Interactions*
  • Humans
  • Membrane Transport Proteins / metabolism*


  • Membrane Transport Proteins