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Research indicates that cholestasis leads to alterations in both hepatic and extrahepatic DMETs, with changes in expression and function documented in rodents and humans. This review synthesizes the modifications in key drug disposition components within cholestasis, focusing on cytochrome P450 (CYP450), drug transporters, and their substrates. Additionally, we briefly discuss certain drugs that have demonstrated efficacy in restoring DMET expression in cholestatic conditions. Ultimately, these insights necessitate a reevaluation of drug selection and dosing guidelines for patients with cholestasis.<\/jats:p>","DOI":"10.1002\/prp2.1220","type":"journal-article","created":{"date-parts":[[2024,6,20]],"date-time":"2024-06-20T10:39:19Z","timestamp":1718879959000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Drug disposition in cholestasis: An important concern"],"prefix":"10.1002","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0009-0006-6347-2023","authenticated-orcid":false,"given":"Tianze","family":"Shang","sequence":"first","affiliation":[{"name":"Department of Pharmacy, Tongji Hospital, Tongji Medical College Huazhong University of Science and Technology  Wuhan 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