Why Clinical Modulation of Efflux Transport at the Human Blood-brain Barrier is Unlikely: the ITC Evidence-based Position

Overview

Journal Clin Pharmacol Ther

Publisher Wiley

Specialty Pharmacology

Date 2013 Apr 17

PMID 23588303

Citations 83

Authors

J C Kalvass

J W Polli

D L Bourdet

B Feng

S-M Huang

X Liu

Q R Smith

L K Zhang

M J Zamek-Gliszczynski

Affiliations

Soon will be listed here.

Abstract

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.

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