ADME DMPK Assays

With respect to drug absorption, transport and metabolism, Ussing chambers are recognized as the gold standard in vitro method. By allowing investigations in living tissues, our ADME/DMPK assays models can accurately predict drug behavior in humans.

Oral bioavailability is dependent not only on liver metabolism but also, critically, on absorption through the gastrointestinal tract, where passive and active absorption and metabolism via brush-border enzymes are key.  Alternative in vitro methods, such as Caco-2 cells or intestinal microsomes, are useful for either permeability or metabolism experiments, but not for both. This is because they don't express the correct levels of transporters or enzymes; only human fresh tissues reflect the true biology.

Moreover, as many animal species used in preclinical species differ significantly in their patterns of gastrointestinal permeability or metabolism, using human fresh gastrointestinal tissue avoids species differences when predicting oral bioavailability.

Ussing Chamber digram-1

Diagram showing the typical setup of an ADME/DMPK experiment in our Ussing Chamber model


Gastrointestinal permeability 

Our permeability studies use human gastrointestinal (GI) tissues which have a phenotypically accurate balance of drug-metabolizing enzymes and transporters. A typical experiment involves the application of a drug to the apical surface of the tissue, followed by periodic sampling of the Ussing chambers to measure the passage of drugs and any metabolites.

  • Between 6-12 biopsies available per donor
  • Healthy and diseased (inflammatory bowel disease) tissues can be used
  • Three reference control compounds compared to test article
  • Provides the closest method to testing your drug in the clinic
  • Option to conduct studies in accordance with GLP

Ussing chamber close up

Close-up of one of our scientists operating an Ussing chamber in our Glasgow laboratory.

Permeability in IBD tissues
This model uses gut biopsies from IBD donors to assess the gastrointestinal permeability of your test articles. 

IBD permeability model →

Permeability in healthy intestine
This model uses gut biopsies from healthy donors to assess the gastrointestinal permeability of your test articles. 

Heathy GI permeability model →


Gastrointestinal metabolism

In addition to our permeability model, we can also estimate gastrointestinal metabolism in our Ussing chamber system. By choosing to predict drug metabolism in living human tissues you can negate the metabolic and species differences presented by Caco-2 and animal models.

  • Up to 12 isolated tissue preparations per donor
  • Metabolism due to both Phase 1 and Phase 2 enzymes can be measured
  • Multiple drugs can be investigated in each experiment
  • Provides the closest method to testing your drug in the clinic

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One of our scientists operating an Ussing chamber in our Glasgow laboratory.

Gastrointestinal metabolism in human fresh tissues
This assay uses gastrointestinal biopsies to investigate the effects of your test article on Phase1 and Phase 2 metabolic enzymes.

Healthy GI metabolism model →


Ion channel function

If you are interested in investigating ion channel function, our Ussing chamber system can be used to detect changes in channel activity or exchange mechanisms. By measuring short circuit current (Isc, µAmps), we can predict the effect of your test articles on ion channel function in gastrointestinal tissues, where ion channels play a large role in regulating fluid secretion.

  • Compounds are tested in duplicate at six concentrations
  • Various regions of the gastrointestinal tract are available 
  • Assays available for sodium channels, chloride channels and adrenoceptors 

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One of our scientists operating an Ussing chamber in our Glasgow laboratory.

Sodium channel function
This assay uses tracheal mucosa to assess the effects of your test article on sodium channels in the respiratory system.

Sodium channel model →

Chloride channel function
This assay uses intestinal mucosa to assess the effects of your test article on chloride channels in the gastrointestinal tract.

Chloride channel model →


Have questions about our ADME DMPK studies? Fill in the form below to contact our human tissue experts.