In vitro Assay to Determine the Intrinsic Clearance of Slowly Metabolized Compounds via Human HUREL Micro Livers
A low clearance Clint high-throughput assay using HUREL Micro Livers (Visikol) was designed to efficiently predict in vivo clearance of slowly metabolized compounds. Low clearance is essential for successful drug discovery outcomes. However, it raises challenges to determine the metabolic clearance in vitro to enable the prediction of human pharmacokinetics.
In this poster, you can find out more about:
- The in vitro methodology applied to determine the in vitro clearance of slowly metabolized compounds in HUREL micro-livers
- Determination of fraction unbound in the incubation (Fuinc)
- Calibration of the clearance assay to enable the prediction of in vivo human clearance by determining a regression offset
- Comparison of predicted unbound Clint values with values derived from literature data, showing predictions within 2-fold