How to Get Drugs Into the Brain
Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Recently, Dennis Koester gave us a crash course in CNS drug discovery in a Drug Hunter Flash Talk. Here, he sums up some key points on how to find compounds that cross the blood-brain barrier, including:
How to Get Drugs Into the Brain
The Blood-Brain Barrier, Gatekeeper of the Brain
What Makes a Compound Brain-Penetrant?
Aim for High Passive Permeability While Avoiding Efflux Transporters
What is Kp,uu? Why Kp,uu is the Most Important Parameter in CNS Drug Discovery
What Influences the Kp,uu of Drugs?
Tools for Predicting Brain Penetration
In Vitro Assays for Evaluating Permeability and Efflux
Harnessing In Silico and In Vitro Data to Predict Kp,uu in CNS Drug Discovery
Optimize for Unbound Brain Concentration, not Unbound Fraction
Examples of Improved Brain Exposure from CNS Drug Discovery
Key Guidelines for CNS Drug Discovery
How to Get Drugs Into the Brain
