Demystifying brain penetration in central nervous system drug discovery: Miniperspective
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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. Key parameters for brain penetration are discussed, including unbound brain concentration, unbound brain-to-plasma ratio, BBB permeability, fraction unbound in brain and plasma, and transporters. Results from a retrospective analysis of 32 Pfizer CNS clinical drug candidates are described. Frequently encountered misconceptions about brain penetration …
