In Vitro Metabolic Stability Studies for Drug Discovery & Development
Metabolic stability studies in drug discovery and development assess the ability of a compound to be metabolized by enzymes through biotransformation. Measurement of intrinsic clearance rates can inform the pharmacokinetic profile of an investigative compound and allow drug developers to select an animal species with the closest metabolic profile to humans for nonclinical testing so as to better predict behavior in patients.
Our Approach to Metabolic Stability Assays
Metabolic stability studies are not specifically required per regulatory guidance, but they can be helpful to identify appropriate species for nonclinical animal studies. Our contract service assesses the stability of a compound by measuring the disappearance of the parent compound in the selected in vitro test system.
- LC-MS method development for analysis of test article
- Triplicate measurements of compound incubated with an appropriate test system and cofactor at multiple time points.
- Negative controls included are zero-time and zero-cofactor samples
- A positive control substrate (e.g., 7-ethoxycoumarin, midazolam) is included to confirm metabolic competency of the test system
- Tabular data summary
Test Systems We Offer (available in human and various animal species)
*Certain extrahepatic test systems may be available upon request.
Related Service: Metabolic Stability Screening
Discovery Plus™ Screening Suite presents medium-throughput alternatives to definitive metabolism & DDI studies through non-GLP, condensed versions of our definitive metabolic stability assays. This option is best used for comparison of multiple compounds or to yield preliminary data for definitive in vitro studies.