Caco-2 permeable


  • Caco-2 permeability

Caco-2 refers to human colon epithelial cancer cells which are used as a model of human intestinal absorption of drugs. These cells are used due to the fact that when cultured, they form tight junctions between cells which makes them resemble the paracellular movement of compounds across the monolayer. Additionally, Caco-2 cells are known to express transporter proteins, efflux proteins, and conjugation enzymes that are common pathways for transcellular entering and metabolic transformation of external substances. Hence, the testing in Caco-2 permeability is an indirect measure of human intestinal absorption.2

In DrugBank, it is possible to find the experimental and predicted values for Caco-2 permeability.

In the predicted ADMET features found in DrugBank, the Caco-2 permeability property is produced using the prediction software admetSAR 1 and the terms found in the table on the drug card should be considered as follows:

Value - it can be presented by  " + " or " - " indicating a yes or no relationship for the predicted property.
Probability - it presents a number between 0-1 and it indicates the certainty of the value describing the ADMET property of this drug based on the prediction software. 

For example, "There is a 82.85% probability that the drug X is permeable through Caco-2 cells based on the prediction of admetSAR software."


  1. Cheng F, Li W, Zhou Y, Shen J, Wu Z, Liu G, Lee PW, Tang Y: admetSAR: a comprehensive source and free tool for assessment of chemical ADMET properties. J Chem Inf Model. 2012 Nov 26;52(11):3099-105. doi: 10.1021/ci300367a. Epub 2012 Nov 1. [Article]
  2. van Breemen RB, Li Y: Caco-2 cell permeability assays to measure drug absorption. Expert Opin Drug Metab Toxicol. 2005 Aug;1(2):175-85. doi: 10.1517/17425255.1.2.175 . [Article]
  3. Signature discovery [Link]