The effect of gut microbiota on drug metabolism

Expert Opin Drug Metab Toxicol. 2013 Oct;9(10):1295-308. doi: 10.1517/17425255.2013.807798. Epub 2013 Jun 12.


Introduction: Numerous drugs and toxicants must be metabolized to an active form. Metabolic activation by host tissues, such as the liver, has been well studied. However, drug and toxicant metabolism by the intestinal microbiota is an unexplored, but essential, field of study in pharmacology and toxicology. The taxonomic diversity and sheer numbers of the intestinal microbiota, and their capacity to metabolize xenobiotics, underscore the importance of this mode of metabolism.

Areas covered: Metabolism by the intestinal microbiota has focused on the natural products of glycosides hydrolyzed by intestinal microbiota enzymes, but not by host tissues. Metabolism of synthetic drugs by the intestinal microbiota has been less-intensively investigated. This review provides an overview of xenobiotic metabolism by the intestinal microbiota of both natural products and synthetic drugs.

Expert opinion: Metabolism by the intestinal microbiota might result in a different metabolite profile than that produced by host tissues. This could potentially result in either activation or inactivation of the pharmacological and/or toxicological actions of the compound in question. The contribution of the intestinal microbiota to drug metabolism remains relatively unexplored. Therefore, studies of xenobiotic metabolism by the intestinal microbiota need to be included in new drug development as well as classical studies of host tissue metabolism.

Publication types

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

MeSH terms

  • Animals
  • Gastrointestinal Tract / drug effects*
  • Gastrointestinal Tract / microbiology*
  • Humans
  • Liver / drug effects
  • Liver / metabolism
  • Microbiota*
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / metabolism*
  • Xenobiotics / pharmacokinetics*


  • Pharmaceutical Preparations
  • Xenobiotics