The Caco-2 cell monolayer: usefulness and limitations

Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):395-411. doi: 10.1517/17425255.4.4.395.


Background: The Caco-2 monolayer has been used extensively for the high-throughput screening of drug permeability and identification of substrates, inhibitors, and inducers of intestinal transporters, especially P-glycoprotein (P-gp). Traditionally, the Caco-2 monolayer is viewed as a single barrier rather than a polarized cell monolayer consisting of metabolic enzymes that are sandwiched between two membrane barriers with distinctly different transporters.

Objective: This review addressed the usefulness and limitations of the Caco-2 cell monolayer in drug discovery and mechanistic studies.

Methods: This mini-review covered applications of the Caco-2 monolayer, clarified misconceptions, and critically addressed issues on data interpretation.

Conclusion: The catenary model extends the usefulness of Caco-2 monolayer and provides proper mechanistic insight and data interpretation.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Biological Transport
  • Caco-2 Cells
  • Humans
  • Models, Biological
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics*


  • Pharmaceutical Preparations