Abstract
Increasing evidence uncovers the involvement of gut microbiota in the metabolism of numerous pharmaceutical drugs. The human gut microbiome harbors 10–100 trillion symbiotic gut microbial bacteria that use drugs as substrates for enzymatic processes to alter host metabolism. Thus, microbiota-mediated drug metabolism can change the conventional drug action course and cause inter-individual differences in efficacy and toxicity, making it vital for drug discovery and development. This review focuses on drug biotransformation pathways and discusses different models for evaluating the role of gut microbiota in drug metabolism.
SIGNIFICANCE STATEMENT This review emphasizes the importance of gut microbiota and different modes of drug metabolism mediated by them. It provides information on in vivo, in vitro, ex vivo, in silico and multi-omics approaches for identifying the role of gut microbiota in metabolism. Further, it highlights the significance of gut microbiota-mediated metabolism in the process of new drug discovery and development as a rationale for safe and efficacious drug therapy.
Footnotes
- Received December 27, 2021.
- Accepted September 8, 2021.
This work received no external funding.
No author has an actual or perceived conflict of interest with the contents of this article.
- Copyright © 2022 by The American Society for Pharmacology and Experimental Therapeutics
DMD articles become freely available 12 months after publication, and remain freely available for 5 years.Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page.
|
Log in using your username and password
Purchase access
In this issue
Drug Metabolism by the Gut Microbiota
Jump to section
- Article
- Visual Overview
- Abstract
- 1. Introduction
- 2. Gut Microbiota: Composition and Physiologic Functions
- 3. Drug Metabolism by the Gut Microbiota
- 4. Modes of Drug Metabolism by the Gut Microbiota
- 5. Experimental Approaches to Analyze the Metabolism of Drugs by Gut Microbiota
- 6. Toxicological Assessment of Drug Metabolites
- 7. Impact of Drugs on the Gut Microbiome
- 8. Conclusion
- Acknowledgments
- Authorship Contribution
- Footnotes
- Abbreviations
- References
- Figures & Data
- Info & Metrics
- eLetters