Book excerpt: 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 in one of the mostsignificant – and most challenging – areas of drugdiscovery. • Written by world experts to provide practicalsolutions to increase brain penetration or minimize CNSside-effects • Reviews state-of-the-art in silico, in vitro, and invivo tools to assess brain penetration and advanced CNS drugdelivery strategies • Covers BBB physiology, medicinal chemistry designprinciples, free drug hypothesis for the BBB, and transportmechanisms including passive diffusion, uptake/efflux transporters,and receptor-mediated processes • Highlights the advances in modelling BBBpharmacokinetics and dynamics relationships (PK/PD) andphysiologically-based pharmacokinetics (PBPK) • Discusses case studies of successful CNS and non-CNSdrugs, lessons learned and paths to the market