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Two transplant cases illustrates the impact of rifampin on tacrolimus pharmacokinetics. In one case, the tacrolimus dosage had to be increased to 120\u2009mg\/day during rifampin coadministration to maintain therapeutic concentrations, with a concentration\u2010to\u2010dose ratio (CDR) as low as 0.11\u2009\u03bcg\/L\/mg. In both cases, cessation of rifampin led to a delayed but significant rise in tacrolimus levels, requiring substantial dose reductions within 7\u201315\u2009days. These cases highlight the extreme variability in tacrolimus metabolism under the influence of rifampin and emphasize the need for daily therapeutic drug monitoring when starting, continuing and discontinuing rifampin. A multidisciplinary approach is essential and, when possible, the tacrolimus\u2013rifampin combination should be avoided.<\/jats:p>","DOI":"10.1002\/bcp.70298","type":"journal-article","created":{"date-parts":[[2025,9,30]],"date-time":"2025-09-30T14:00:10Z","timestamp":1759240810000},"page":"3542-3548","source":"Crossref","is-referenced-by-count":3,"title":["Challenges in optimizing tacrolimus therapy in patients treated with rifampin: A case series"],"prefix":"10.1002","volume":"91","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5521-2519","authenticated-orcid":false,"given":"Jeroen P. A.","family":"Houwen","sequence":"first","affiliation":[{"name":"Department of Clinical Pharmacy University Medical Center Utrecht and Utrecht University  Utrecht The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Aurelia H. 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