Drug metabolism

Rapid metabolism is a major limiting feature of many new drug candidates. It can lead to low oral bioavailability, a short in vivo half-life or the production of potentially active or toxic metabolites.

CDCO offers a range of standard and custom-designed assays to assess the metabolism of compounds during lead optimisation and preclinical development.

Metabolite characterisation studies are performed to:

  • identify major metabolic products and metabolising enzymes of a test compound
  • identify metabolically labile functional moieties within a structural series
  • provide a basis for structural modifications to reduce metabolic liabilities

Research platforms include:

  • metabolic stability using liver microsomes or cryopreserved hepatocytes
  • metabolite identification and characterisation
  • species comparisons of metabolite profiles
  • CYP and UGT reaction phenotyping
  • stability in blood and/or plasma
  • stability in gastric and intestinal fluids
  • glutathione conjugate/reactive metabolite detection