Why clinical modulation of efflux transport at the human blood-brain barrier is unlikely: the ITC evidence-based position

Clin Pharmacol Ther. 2013 Jul;94(1):80-94. doi: 10.1038/clpt.2013.34. Epub 2013 Feb 14.


Drug interactions due to efflux transport inhibition at the blood-brain barrier (BBB) have been receiving increasing scrutiny because of the theoretical possibility of adverse central nervous system (CNS) effects identified in preclinical studies. In this review, evidence from pharmacokinetic, pharmacodynamic, imaging, pharmacogenetic, and pharmacovigilance studies, along with drug safety reports, is presented supporting a low probability of modulating transporters at the human BBB by currently marketed drugs.

Publication types

  • Review

MeSH terms

  • Biological Transport / physiology
  • Blood-Brain Barrier / metabolism*
  • Drug Design
  • Drug Evaluation, Preclinical
  • Drug Interactions*
  • Humans
  • Membrane Transport Proteins / metabolism*
  • Pharmaceutical Preparations*
  • Pharmacokinetics


  • Membrane Transport Proteins
  • Pharmaceutical Preparations