Mechanistic Understanding of Brain Drug Disposition to Optimize the Selection of Potential Neurotherapeutics in Drug Discovery

Utility of CSF in translational neuroscience

(2013) Elizabeth C. M. de Lange   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

Drug-drug interactions involving lysosomes: mechanisms and potential clinical implications

(2012) Randall Logan et al.   Expert Opinion on Drug Metabolism & Toxicology

Demystifying Brain Penetration in Central Nervous System Drug Discovery

(2012) Li Di et al.   JOURNAL OF MEDICINAL CHEMISTRY

Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery

(2011) Arup K. Ghose et al.   ACS Chemical Neuroscience

Comparative psychology and the grand challenge of drug discovery in psychiatry and neurodegeneration

(2011) Dani Brunner et al.   BEHAVIOURAL PROCESSES

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

Robust Central Reduction of Amyloid-  in Humans with an Orally Available, Non-Peptidic  -Secretase Inhibitor

(2011) P. C. May et al.   JOURNAL OF NEUROSCIENCE

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

Modulation of Mrp1 (ABCc1) and Pgp (ABCb1) by Bilirubin at the Blood-CSF and Blood-Brain Barriers in the Gunn Rat

(2011) Silvia Gazzin et al.   PLoS One

Associatingin vitrotarget binding andin vivoCNS occupancy of serotonin reuptake inhibitors in rats: The role of free drug concentrations

(2011) Christoffer Bundgaard et al.   XENOBIOTICA

Trends in Risks Associated With New Drug Development: Success Rates for Investigational Drugs

(2010) J A DiMasi et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Pharmaceutical Innovation in the 21st Century: New Drug Approvals in the First Decade, 2000–2009

(2010) K I Kaitin et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Measurement of Unbound Drug Exposure in Brain: Modeling of pH Partitioning Explains Diverging Results between the Brain Slice and Brain Homogenate Methods

(2010) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Assessing brain free fraction in early drug discovery

(2010) Kevin D Read et al.   Expert Opinion on Drug Metabolism & Toxicology

Active-Site Concentrations of Chemicals - Are They a Better Predictor of Effect than Plasma/Organ/Tissue Concentrations?

(2009) Margareta Hammarlund-Udenaes   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Addressing Central Nervous System (CNS) Penetration in Drug Discovery: Basics and Implications of the Evolving New Concept

(2009) Andreas Reichel   CHEMISTRY & BIODIVERSITY

Methodologies to Assess Brain Drug Delivery in Lead Optimization

(2009) Margareta Hammarlund-Udenaes et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Receptor Occupancy and Brain Free Fraction

(2009) J. Watson et al.   DRUG METABOLISM AND DISPOSITION

Unbound Brain Concentration Determines Receptor Occupancy: A Correlation of Drug Concentration and Brain Serotonin and Dopamine Reuptake Transporter Occupancy for Eighteen Compounds in Rats

(2009) X. Liu et al.   DRUG METABOLISM AND DISPOSITION

Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System

(2009) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Improved Measurement of Drug Exposure in the Brain Using Drug-Specific Correction for Residual Blood

(2009) Markus Fridén et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Structure−Brain Exposure Relationships in Rat and Human Using a Novel Data Set of Unbound Drug Concentrations in Brain Interstitial and Cerebrospinal Fluids

(2009) Markus Fridén et al.   JOURNAL OF MEDICINAL CHEMISTRY

CSF as a Surrogate for Assessing CNS Exposure: An Industrial Perspective

(2008) Jiunn Lin   CURRENT DRUG METABOLISM

Unbound Drug Concentration in Brain Homogenate and Cerebral Spinal Fluid at Steady State as a Surrogate for Unbound Concentration in Brain Interstitial Fluid

(2008) X. Liu et al.   DRUG METABOLISM AND DISPOSITION

Progress in Brain Penetration Evaluation in Drug Discovery and Development

(2008) X. Liu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS