Investigation of CYP3A induction by PF‐05251749 in early clinical development: comparison of linear slope physiologically based pharmacokinetic prediction and biomarker response

• Main Authors: Jian Lin (Author), Francois Gaudreault (Author), Nathaniel Johnson (Author), Zhiwu Lin (Author), Parya Nouri (Author), Theunis C. Goosen (Author), Aarti Sawant‐Basak (Author)
• Format: Book
• Published: Wiley, 2022-09-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Abstract PF‐05251749 is a dual inhibitor of casein kinase 1 δ/ε under clinical development to treat disruption of circadian rhythm in Alzheimer's and Parkinson's diseases. In vitro, PF‐05251749 (0.3-100 μM) induced CYP3A in cryopreserved human hepatocytes, demonstrating non‐saturable, dose...