Prediction of Intestinal First-Pass Drug Metabolism
Abstract
Despite a lower content of many drug metabolising enzymes in the intestinal epithelium compared to the liver (e.g. intestinal CYP3A abundance in the intestine is 1% that of the liver), intestinal metabolic extraction may be similar to or exceed hepatic extraction. Modelling of events on first-pass through the intestine requires attention to the complex interplay between passive permeability, active transport, binding, relevant blood flows and the intrinsic activity and capacity of enzyme systems. We have compared the predictive accuracy of the "well-stirred" gut model with that of the "Q(Gut)" model. The former overpredicts the fraction escaping first-pass gut metabolism; the latter improves the predictions by accounting for interplay between permeability and metabolism.
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Initial studies of predicting intestinal metabolism focused on CYP3A4, possibly because of the utility of grapefruit juice studies in generating data to assess predictions.
“Initial studies of predicting intestinal metabolism focused on CYP3A4, possibly because of the utility of grapefruit juice studies in generating data to assess predictions [64].”
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Cited by 366
- Authors
- Yang, J., Jamei, M., Yeo, K., Tucker, G., & Rostami-Hodjegan, A.
- Affiliations
- Simcyp (United Kingdom) (GB)
- Venue
- Current Drug Metabolism
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2007-10-01
- Volume
- 8
- Issue
- 7
- Pages
- 676-684
- ISSN
- 1389-2002 (ISSN-L)
- OpenAlex
- W2124945212
- Cited by
- 366
- References
- 0
- Citations by year
- 2026: 12 · 2025: 18 · 2024: 18 · 2023: 10 · 2022: 17 · 2021: 19 · 2020: 17 · 2019: 16 · 2018: 19 · 2017: 20 · 2016: 29 · 2015: 14 · 2014: 21 · 2013: 24 · 2012: 28
- FWCI
- 18.02
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Drug Metabolism (publishedVersion)
- PubMed (publishedVersion)
- Research Explorer (The University of Manchester) (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- intestinal first-pass metabolism, drug metabolism prediction, active transport, drug binding, blood flow, hepatic extraction
- MeSH terms
- Administration, Oral, Animals, Biotransformation, Pharmaceutical Preparations, Forecasting, Humans, Intestinal Absorption, Intestinal Mucosa, Models, Biological
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