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How To Predict Oral Absorption Of Your Test Compound With High Quality In Vitro Data?

Author: Iontox Biotechnology
by Iontox Biotechnology
Posted: May 23, 2020

The Caco-2 permeability assay has become the gold standard in vitro method to assess a test compound’s readiness for oral dosing.

Why to Choose The Caco-2 Permeability Assay?

Solubility and intestinal permeability are the important factors in determining the oral absorption of drugs. By evaluating compound permeability in early drug discovery, organizations can distinguish test compounds which are more likely to cause drug failure in the later stages of drug development due to poor intestinal permeability. Compounds with poor permeability and solubility are not likely to possess the favorable absorption, distribution, metabolism, and excretion parameters (ADME Parameters) for an investigational new drug and may cause drug failure in the clinic.

The Caco-2 permeability assay is a United States FDA recommended in vitro method for the prediction of drug permeability.

One of the key reasons the Caco-2 permeability assay is widely accepted by regulatory bodies is the Caco-2 cell line. The Caco-2 human colon carcinoma cell line has characteristics that mimic human epithelial cells found in the intestine such as the formation of a well-differentiated monolayer of cells containing a defined brush border on the apical surface. This monolayer of cells also contains many of the brush border enzymes that mediate the active uptake or ef?ux of drugs in the human intestine.

Because of the Caco-2 cell line’s ability to mimic human intestinal epithelial cells, the in vivo absorption of a compound in the intestine can be predicted by assessing the transport rate of a compound across a Caco-2 cell monolayer membrane. Additional assessments can be made, including whether a test compound is actively transported by P-glycoprotein (P-gp).

Key Points About The Caco-2 Permeability Assay

  • The Caco-2 permeability assay is an FDA recommended assay for companies applying for an Investigational New Drug (IND).
  • The Caco-2 assay is utilized as an in vitro study for the human intestinal absorption of drugs.
  • When run with a reliable CRO, the Caco-2 permeability assay can predict the suitability of your test compound for oral dosing.
  • Additional assessments that can be made when running the Caco-2 permeability assay including an analysis on whether a test compound is actively transported by P-glycoprotein (P-gp).

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

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

Choose a professional CRO, which offers quality drug discovery services and provides guidance and support to clients for the discovery and development of novel drugs.

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

To learn more about the Caco-2 permeability assay, visit https://www.iontox.com/caco-2-permeability-assay/ today.

About the Author

IONTOX is a biotechnology company founded in 2014 dedicated to providing expertise to the area of in vitro toxicology, with a mission to build improved methods for predicting human adverse effects from chemical..

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Author: Iontox Biotechnology

Iontox Biotechnology

Member since: Feb 28, 2020
Published articles: 2

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