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 specific requirements. We support your projects in setting up your studies to meet regulatory requirements.

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

Physico-chemical Parameters

  • Storage
  • Chemical stability
  • Lipophilicity
  • Aqueous solubility

Stability in Biological Matrices

  • Blood
  • Plasma
  • Intestinal fluids
  • Further matrices on request

Membrane Permeability

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

Interaction with Drug Transporters

  • ABC-ATP binding
  • SLC transporters* (inhibition/uptake)
  • PgP interaction
  • *in cooperation

Protein Binding Mechanism

  • PPB
  • SPB
  • Blood partitioning
  • Kd (HSA, AGP)
  • Microsomal binding

Brain Tissue Binding

  • Rat, mice tissue
  • Ultrafiltration

Metabolic Stability

  • Liver microsomes
  • S9
  • Hepatocytes
  • UGT profiling

Reactive Metabolite Trapping

  • Liver microsomes
  • GSH
  • SCZ
  • Orbitrap technology

Metabolite Identification

  • Liver microsomes
  • S9
  • Hepatocytes
  • Orbitrap technology
  • Metabolic pathway
  • Metabolite abundance

CYP Inhibition

  • Liver microsomes
  • Hepatocytes
  • Recombinant human CYPs
  • Mode of inhibition, inhibition kinetics

CYP Induction

  • 2D & 3D human hepatocytes
  • Hepa RG┬«
  • Functional activity
  • mRNA*

*in cooperation

CYP Phenotyping

  • Recombinant human CYPs
  • Loss of parent compound
  • Clint
  • Half-life

Further assays are available on request. In addition to the standard setup, all assays are also offered in a fit-for-screening format. Screening assay packages will be tailored to your project┬┤s requirement.

Please contact us for your specific ADME study!

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

Dr. Ursula Mueller-Vieira
Head of ADMET & in vitro Pharmacology
mueller@pharmacelsus.de