Assessment of the blood–brain barrier in CNS drug discovery

P Jeffrey, S Summerfield - Neurobiology of disease, 2010 - Elsevier
A wide variety of models have been developed over the years to predict blood–brain barrier
(BBB) penetration, most of them have focussed on predicting total concentrations of drug …

Assays to predict drug permeation across the blood-brain barrier, and distribution to brain

NJ Abbott, DEM Dolman… - Current drug …, 2008 - ingentaconnect.com
Drug discovery programmes to target or avoid the brain need to take into account the
properties of the blood-brain barrier (BBB). The importance to CNS PK of the free drug …

[图书][B] Blood-brain barrier in drug discovery: optimizing brain exposure of CNS drugs and minimizing brain side effects for peripheral drugs

L Di, EH Kerns - 2015 - books.google.com
Focused on central nervous system (CNS) drug discovery efforts, this book educates drug
researchers about the blood-brain barrier (BBB) so they can affect important improvements …

Current in vitro and in silico models of blood-brain barrier penetration: a practical view.

M Vastag, GM Keseru - Current opinion in drug discovery & …, 2009 - europepmc.org
Predictive, cost effective and fast evaluation of CNS penetration or unbound brain levels of
NCEs, or both, presents a considerable challenge in preclinical screening in the …

Preclinical prediction of human brain target site concentrations: considerations in extrapolating to the clinical setting

J Westerhout, M Danhof, ECM De Lange - Journal of pharmaceutical …, 2011 - Elsevier
The development of drugs for central nervous system (CNS) disorders has encountered high
failure rates. In part, this has been due to the sole focus on blood-brain barrier permeability …

Demystifying brain penetration in central nervous system drug discovery: Miniperspective

L Di, H Rong, B Feng - Journal of medicinal chemistry, 2013 - ACS Publications
This Perspective provides important concepts about the blood–brain barrier (BBB) in drug
discovery and how they should be applied effectively in designing successful CNS drugs …

Prediction of blood–brain barrier permeation in drug discovery from in vivo, in vitro and in silico models

NJ Abbott - Drug Discovery Today: Technologies, 2004 - Elsevier
The properties of the blood–brain barrier (BBB) are important considerations when
designing drugs to target or avoid the brain. In vivo models provide some of the most reliable …

Drug penetration across the blood–brain barrier: an overview

V Mangas-Sanjuan, M González-Alvarez… - Therapeutic …, 2010 - Taylor & Francis
The brain is one of the most protected organs in the body. There are two key barriers that
control the access of endogenous substances and xenobiotics (drugs or toxins) to the CNS …

[HTML][HTML] Mimicking brain tissue binding in an in vitro model of the blood-brain barrier illustrates differences between in vitro and in vivo methods for assessing the rate …

M Heymans, E Sevin, F Gosselet, S Lundquist… - European Journal of …, 2018 - Elsevier
Assessing the rate of drug delivery to the central nervous system (CNS) in vitro has been
used for decades to predict whether CNS drug candidates are likely to attain their …

Translational aspects of blood–brain barrier transport and central nervous system effects of drugs: from discovery to patients

ECM De Lange… - Clinical Pharmacology & …, 2015 - Wiley Online Library
The development of CNS drugs is associated with high failure rates. It is postulated that too
much focus has been put on BBB permeability and too little on understanding BBB transport …