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Pharmacelsus

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

  • PAMPA
  • 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!

Dr. Stephanie Urschel
Head of Business Development & Sales
urschel@pharmacelsus.de

Dr. Julia Przibilla
Team Manager ADMET & in vitro Pharmacology
przibilla@pharmacelsus.de

Pharmacelsus GmbH
Science Park 2
66123 Saarbruecken / Germany

Phone: +49 (0)681 3946 7510
Email:  info@pharmacelsus.de