Reliability of in vitro data for the mechanistic prediction of brain extracellular fluid pharmacokinetics of P-glycoprotein substrates in vivo; are we scaling correctly?
Daan Willem van Valkengoed,
Makoto Hirasawa,
Vivi Rottschäfer
et al.
Abstract:Plasma pharmacokinetic (PK) profiles often do not resemble the PK within the central nervous system (CNS) because of blood-brain-border (BBB) processes, like active efflux by P-glycoprotein (P-gp). Methods to predict CNS-PK are therefore desired. Here we investigate whether in vitro apparent permeability (Papp) and corrected efflux ratio (ERc) extracted from literature can be repurposed as input for the LeiCNS-PK3.4 physiologically-based PK model to confidently predict rat brain extracellular fluid (ECF) PK of… Show more
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