In vitro ADME Screening

Charles River provides comprehensive ADME services which can be accessed as part of an integrated drug discovery program, or as a stand-alone offering. With extensive knowledge of in vitro ADME gained through working within drug discovery environments at both pharmaceutical and biotech companies, our ADME experts offer a consultative approach, ensuring that the right experiments are performed at the right time.

With multiple formats available for many of our in vitro assays to suit the different stages of the drug discovery pipeline, we offer a flexible approach to our ADME services. Validated, SOP-controlled assays are available in addition to assay protocols and final reports tailored to the specific needs of a client. We are happy to discuss the adoption of client's own protocols for any assay of interest.

Physicochemical Properties

  • Kinetic solubility
  • Thermodynamic solubility
  • Lipophilicity
  • Chemical stability

Metabolic Stability

  • Microsomes (both lung and liver)
  • S9 fraction (intestinal, lung and liver)
  • Cryopreserved hepatocytes
  • P450 isoforms
  • UGT isoforms
  • Plasma
  • Blood
  • Simulated intestinal/gastric fluids

Drug-drug Interactions

  • CYP450 inhibition: fluorescence based
  • CYP450 inhibition: mass spectrometry based
  • Time-dependent CYP450 inhibition
  • CYP450 induction

Detailed Metabolic Studies

  • Metabolite identification
  • Reaction phenotyping
  • Reaction kinetics (Vmax, Km)

Distribution

  • Plasma protein binding
  • Blood partitioning
  • Caco-2 permeation studies
  • MDR1-MDCK effective efflux
  • BCRP-MDCK effective efflux
  • Pgp ATPase
  • Permeation studies
  • Brain tissue binding
  • Lung tissue binding

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