Wednesday 14 October 2020

Predict Your Test Compound Suitability for Oral Dosing with Caco-2 Permeability Assay


Caco-2 cells are highly useful for intestinal absorption studies due to their ability to model human absorption characteristics. The Caco-2 assay is widely utilized in drug discovery for assessment of compound permeability properties. 

Caco-2 Permeability

Using the caco-2 cell line to assess compound permeability you will be able to differentiate compounds which are likely to pose challenges during preclinical and clinical development. Test compounds with poor permeability are more likely to have poor Absorption, Distribution, Metabolism, Excretion (ADME) and Pharmacokinetics (PK) properties.

When Caco-2 cells are cultured as a monolayer, this human colon carcinoma cell line forms characteristics that mimic intestinal epithelial cells, such as the formation of a polarized monolayer with an apical brush border, which forms tight junctions. This apical brush border contains many of the enzymes and transport proteins that mediate the active uptake or efflux of drugs and chemicals in the intestine.


By assessing the transport rate of a compound across a Caco-2 cell monolayer membrane, the in vivo absorption of the compound across the gut wall can be predicted.

Key Points about Caco-2 Permeability Assay are:

  • The Caco-2 permeability is an FDA recommended assay for organizations applying for an Investigational New Drug (IND). It is utilized as a model of human intestinal absorption of drugs.
  • When run with a reliable CRO, the Caco-2 permeability assay can assess suitability of your test compound for oral dosing.
  • Additional evaluations can be made, including whether a test compound is actively transported by P-glycoprotein (P-gp).

Choosing a Professional Contract Research Organization (CRO) to Run a Caco-2 Study

When looking to run a Caco-2 permeability study, check whether the organization follows GCCP and GIVIMP guidelines. This is a good indicator of experience with in vitro methods and what the quality of the data will be.

IONTOX, L.L.C. is a CRO specializing in vitro methods. IONTOX ‘s Caco-2 permeability assay is overseen by a Diplomat of the American Board of Toxicology and follows the internationally recognized guidance documents on Good In Vitro Method Practices (GIVMP) and Good Cell Culture Practices (GCCP).

For more information regarding Caco-2 permeability assay, visit https://www.iontox.com/caco-2-permeability-assay/ today.

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