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Discovery Plus™ Screening: Metabolic Stability

Our Discovery Plus™ Metabolic Stability assay is a cost-effective, medium-throughput design ideal for non-GLP screening of multiple compounds with regard to estimating in vitro clearance. Microsomal stability (other standard test systems are also available, such as S9) provides a sponsor with initial drug metabolism data for definitive studies.

This medium-throughput service provides you with more than just a quick screen. The early determination of in vitro drug stability is an essential factor in the estimation of intrinsic clearance. This is important because compounds with favorable pharmacokinetic properties can be selected in the discovery setting for further development. 

Moving quickly through drug discovery and development saves you time and money; get data from a Discovery Plus™ screening study quickly to make risk-based decisions faster and get you through the pipeline more efficiently.

Our Approach to Medium-Throughput Screening to Investigate Microsomal Stability (other test systems available)

This medium-throughput assay is 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™ services are best utilized for compounds that are in the discovery or early development phase. For compounds that need a more thorough evaluation, please see our definitive Metabolic Stability service.

  • Screens are performed at three or four optimal time points, dependent on test system chosen (short-, medium-, long-time course options, to a maximum 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, midazolam)
  • Tabular data summary typically within 10 business days of project start

*Duplicates or more can be performed upon request with modified compound throughput

Plasma protein binding provides important inputs for test article concentration calculations for definitive in vitro studies

Human and Animal In Vitro Test Systems

  • S9
  • Microsomes
  • Hepatocytes
  • Recombinant CYP enzymes
  • Plasma
  • Other industry-standard test systems may be available upon request.

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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See the Science

Check out our poster discussing “High Content Automated Metabolic Stability and CYP Inhibition Cocktail Screening Assays for Early Drug Development”

A Specialty CRO team dedicated to the success of safe drugs for market