Metabolic Stability



Overview

Sekisui XenoTech's Discovery Plus™ Metabolic Stability service is more than just a quick screen. The early determination of in vitro drug metabolic stability is an essential factor in the estimation of in vivo clearance. This is important because compounds with favorable pharmacokinetic properties can be selected in the discovery setting for further development. Sekisui XenoTech's Discovery Plus™ metabolic stability screen is a service designed to meet the needs of drug discovery teams, by screening multiple drug candidates in industry standard test systems (S9, microsomes, etc.) with multiple species and rapid turnaround times.

Discovery Plus™ Metabolic Stability Overview
  • Screens are performed at four optimal time points (short-, medium-, long-time course options, to max of 120 minutes)
  • Simultaneously evaluate batches of 6-8 compounds and a positive control or up to six different species with single determination*
  • Generic LC-MS/MS method utilized with generic internal standards for sample analysis
  • Positive control included upon request (7-ethoxycoumarin)
  • Tabular data summary typically within 10 business days of project start
*Duplicates or more can be performed upon request with modified compound throughput

Discovery Plus™ Metabolic Stability Results
  • Measurements of drug loss over 4 time points
  • Determination of drug half life (t1/2) and elimination rate constant (kel)
  • Estimation of in vitro intrinsic clearance (CLint)
  • Data presented as tabular summary sorted by test system
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Protein Binding
CYP Inhibition
Enzyme Induction
Drug Transporter Inhibition
Cell-Based Permeability
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