Imaging techniques to study drug transporter function in vivo

Pharmacol Ther. 2018 Sep;189:104-122. doi: 10.1016/j.pharmthera.2018.04.006. Epub 2018 Apr 22.


Transporter systems involved in the permeation of drugs and solutes across biological membranes are recognized as key determinants of pharmacokinetics. Typically, the action of membrane transporters on drug exposure to tissues in living organisms is inferred from invasive procedures, which cannot be applied in humans. In recent years, imaging methods have greatly progressed in terms of instruments, synthesis of novel imaging probes as well as tools for data analysis. Imaging allows pharmacokinetic parameters in different tissues and organs to be obtained in a non-invasive or minimally invasive way. The aim of this overview is to summarize the current status in the field of molecular imaging of drug transporters. The overview is focused on human studies, both for the characterization of transport systems for imaging agents as well as for the determination of drug pharmacokinetics, and makes reference to animal studies where necessary. We conclude that despite certain methodological limitations, imaging has a great potential to study transporters at work in humans and that imaging will become an important tool, not only in drug development but also in medicine. Imaging allows the mechanistic aspects of transport proteins to be studied, as well as elucidating the influence of genetic background, pathophysiological states and drug-drug interactions on the function of transporters involved in the disposition of drugs.

Keywords: Magnetic resonance imaging; Membrane transporters; Molecular imaging; Pharmacokinetics; Positron emission tomography; Single photon emission computed tomography.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Diagnostic Imaging / methods*
  • Humans
  • Membrane Transport Proteins / metabolism*
  • Pharmaceutical Preparations / metabolism
  • Pharmacokinetics


  • Membrane Transport Proteins
  • Pharmaceutical Preparations