Prediction of oral drug absorption in humans--from cultured cell lines and experimental animals

Expert Opin Drug Metab Toxicol. 2008 May;4(5):581-90. doi: 10.1517/17425255.4.5.581.


Background: Over the past decade, the use of drug metabolism and pharmacokinetic (DMPK) parameters to optimize selection of candidates for drug development has become one of the primary focuses of research organizations involved in new drug discovery.

Objective: This review will focus on the feasibility of predicting human absorption using data from a cultured Caco-2 cell system and non-clinical animals.

Methods: In-house Caco-2 permeability data were compared with human absorption data from the literature. Animal absorption data obtained from current literature were also compared with human data.

Results/conclusion: Using a combination of rapid in-vivo and in-vitro DMPK screens on a large array of compounds during the lead optimization process has resulted in the streamlined development of compounds that have acceptable DMPK properties. Since it is well recognized that human intestinal absorption cannot be precisely predicted by a single screening assay, it is important to utilize various in-vitro and in-vivo non-clinical studies during lead optimization in drug discovery.

Publication types

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

MeSH terms

  • Animals
  • Caco-2 Cells
  • Cell Line
  • Humans
  • Intestinal Absorption / physiology*
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics
  • Species Specificity


  • Pharmaceutical Preparations