Summary of Studies for Pharmacokinetics, Distribution, and Metabolism in Animals
Study type | Duration | Route of administration | Dose or concentration |
Studies in rats | |||
Preliminary pharmacokinetics | Single dose | Intravenous | 1 mg/kg |
Distribution (brain exposure) | Single dose | Intravenous | 0.1 mg/kg |
Distribution and metabolism in plasma and brain | Single dose | Intravenous | 1 mg/kg |
In vitro studies | |||
Brain and plasma protein binding (interspecies) | 1 μM | ||
In vitro permeation through the caco-2 cell model | 2 μM | ||
Intrinsic clearance in microsomes (interspecies) | 1 μM (rhesus), 5 μM (mouse, rat, and human) | ||
Metabolism in microsomes (interspecies) | 1 μM |