Application of a high‐resolution in vitro human MDR1‐MDCK assay and in vivo studies in preclinical species to improve prediction of CNS drug penetration

• Main Authors: Licong Jiang (Author), Sanjeev Kumar (Author), Marc Nuechterlein (Author), Marissa Reyes (Author), Dao Tran (Author), Clifford Cabebe (Author), Peggy Chiang (Author), James Reynolds (Author), Scott Carrier (Author), Yongkai Sun (Author), Peter Eddershaw (Author), Tanya Hay (Author), Weichao Chen (Author), Bo Feng (Author)
• Format: Book
• Published: Wiley, 2022-02-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Abstract P‐glycoprotein (P‐gp, MDR1) is expressed at the blood-brain barrier (BBB) and restricts penetration of its substrates into the central nervous system (CNS). In vitro MDR1 assays are frequently used to predict the in vivo relevance of MDR1‐mediated efflux at the BBB. It has been well establi...