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In vitro ADME Services

The in vitro ADME team of Pharmacelsus combines professionalism of the pharmaceutical industry with the flexibility to adapt standard assays for your specific challenges. We use a consultative approach to set-up tailor-made assays together with you. Studies are conducted to meet regulatory requirements.

Evaluate the “druggability” of your compounds by the following set of in vitro ADME assays.

Physico-chemical Parameters

  • Chemical stability
  • Aqueous solubility

Stability in Biological Matrices

  • Blood
  • Plasma
  • Intestinal fluids
  • Further matrices on request
  • All preclinical species available

Membrane Permeability

  • Artificial BBB
  • Bidirectional Caco2
  • PgP interaction
  • Nuclear uptake

Interaction with Drug Transporters*

  • ABC-ATP binding
  • SLC transporters: inhibition/uptake
  • PgP interaction

*in cooperation

Protein Binding Mechanism

  • PPB (crossfiltration or Rapid Equilibrium Dialysis)
  • SPB (crossfiltration or Rapid Equilibrium Dialysis)
  • Blood partitioning
  • Microsomal binding

Brain Tissue Binding

  • Rat, mice tissue
  • Ultrafiltration
  • Rapid Equilibrium Dialysis

Metabolic Stability

  • Liver or intestinal microsomes
  • Liver or intestinal S9 fraction
  • Hepatocytes
  • All preclinical species available

Reactive Metabolite Trapping

  • Liver microsomes
  • GSH

Metabolite Identification

  • Liver or intestinal microsomes
  • Liver or intestinal S9 fraction
  • Hepatocytes
  • Metabolic pathway

CYP Inhibition

  • Recombinant human CYPs
  • IC50 determination
  • Human liver microsomes*
  • Mode of inhibition, inhibition kinetics

*according to EMA/FDA Guidelines

CYP Induction

  • Hepa RG®
  • Human hepatocytes
  • Functional activity
  • mRNA

CYP Phenotyping

  • Recombinant human CYPs
  • Loss of parent compound
  • Clint
  • Half-life
  • Formation of major Phase 1 metabolites and metabolic pathway elucidation

Further assays are available on request. All assays can be tailored to project´s requirements and offered in a fit for screening format.

Please contact us for your specific ADME study!

MUDr. Maria Li
Director Business Development

Dr. Julia Przibilla
Team Manager ADMET & in vitro Pharmacology