Imaging techniques to study drug transporter function in vivo
Techniques d'imagerie pour l'étude des transporteurs de médicaments
Résumé
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 noninvasive
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.
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