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Watanabe, Reiko; Esaki, Tsuyoshi; Ohashi, Rikiya; Kuroda, Masataka; Kawashima, Hitoshi; Komura, Hiroshi; Natsume-Kitatani, Yayoi; Mizuguchi, Kenji
Journal of medicinal chemistry, 03/2021, Volume: 64, Issue: 5Journal Article
Developing models to predict the brain penetration of drugs remains a challenge owing to the intricate involvement of multiple transport systems in the blood brain barrier, and the necessity to consider a combination of multiple pharmacokinetic parameters. P-glycoprotein (P-gp) is one of the most important transporters affecting the brain penetration of drugs. Here, we developed an prediction model for P-gp efflux potential in brain capillary endothelial cells (BCEC). Using the representative values of P-gp net efflux ratio in BCEC, we proposed a novel prediction system for brain-to-plasma concentration ratio ( ) and unbound brain-to-plasma concentration ratio ( ) of P-gp substrates. We validated the proposed prediction system using newly acquired experimental brain penetration data of 28 P-gp substrates. Our system improved the predictive accuracy of brain penetration of drugs using only chemical structure information compared with that of previous studies.
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