Set up the metabolic profile of a drug is essential during its development.

Human drug metabolites are increasingly requiring attention due to their impact on pharmacological activity and drug safety. As a result, they need to be assessed at an early stage to identify potential metabolic differences between animals and humans. This helps assess the relevance of animal models for toxicological evaluations and avoids development delays. Using in vitro studies, it is possible to identify metabolites by high-resolution mass spectrometry, to obtain a semi-quantitative estimate of their concentration and to highlight differences in metabolism between species. Two types of service are offered:

  1. Searching for metabolite masses by comparing chromatograms at the beginning and end of the incubation (MS analysis).
  2. In addition to step 1), determine the structure of metabolites identified by fragmentation (MS/MS analysis).

Protocol

SpeciesHuman, rat, mouse, dog, monkey and mini pig
Available matricesPreferably hepatocytes or liver microsomes.
Test concentration10µM
Temperature37°C
Time pointst0 and t = 2h
Analysis methodHigh resolution LC-MS and MS/MS
Data delivery
  1. List of reactions that produced the detected metabolites
  2. Putative structure of metabolites
Replicate3

Notes

It is possible to screen for metabolites proposed by the client and modify the incubation time.

It is better first to check the compound's instability in the presence of liver enzymes.