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| Verfasst von: | Gümüs, Katja S. [VerfasserIn]  |
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| | Teegelbekkers, Anna [VerfasserIn] |
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| | Sauter, Max [VerfasserIn] |
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| | Meid, Andreas [VerfasserIn] |
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| | Burhenne, Jürgen [VerfasserIn] |
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| | Weiß, Johanna [VerfasserIn] |
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| | Blank, Antje [VerfasserIn] |
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| | Haefeli, Walter E. [VerfasserIn] |
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| | Czock, David [VerfasserIn] |
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| Titel: | Effect of tacrolimus formulation (prolonged-release vs immediate-release) on its susceptibility to drug-drug interactions with St. John's Wort |
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| Verf.angabe: | Katja S. Gümüs, Anna Teegelbekkers, Max Sauter, Andreas D. Meid, Jürgen Burhenne, Johanna Weiss, Antje Blank, Walter E. Haefeli, and David Czock |
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| E-Jahr: | 2024 |
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| Jahr: | 04 January 2024 |
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| Umfang: | 10 S. |
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| Fussnoten: | Early view, first published: 04 January 2024 ; Gesehen am 29.02.2024 |
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| Titel Quelle: | Enthalten in: Clinical pharmacology in drug development |
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| Ort Quelle: | Oxford [u.a.] : Wiley-Blackwell, 2012 |
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| Jahr Quelle: | 2024 |
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| Band/Heft Quelle: | 13(2024), Seite 1-10 |
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| ISSN Quelle: | 2160-7648 |
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| Abstract: | Tacrolimus is metabolized by cytochrome P450 3A (CYP3A) and is susceptible to interactions with the CYP3A and P-glycoprotein inducer St. John's Wort (SJW). CYP3A isozymes are predominantly expressed in the small intestine and liver. Prolonged-release tacrolimus (PR-Tac) is largely absorbed in distal intestinal segments and is less susceptible to CYP3A inhibition. The effect of induction by SJW is unknown. In this randomized, crossover trial, 18 healthy volunteers received single oral tacrolimus doses (immediate-release [IR]-Tac or PR-Tac, 5 mg each) alone and during induction by SJW. Concentrations were quantified using ultra-high performance liquid chromatography coupled with tandem mass spectrometry and non-compartmental pharmacokinetics were evaluated. SJW decreased IR-Tac exposure (area under the concentration-time curve) to 73% (95% confidence interval 60%-88%) and maximum concentration (Cmax) to 61% (52%-73%), and PR-Tac exposure to 67% (55%-81%) and Cmax to 69% (58%-82%), with no statistical difference between the 2 formulations. The extent of interaction appeared to be less pronounced in volunteers with higher baseline CYP3A4 activity and in CYP3A5 expressors. In contrast to CYP3A inhibition, CYP3A induction by SJW showed a similar extent of interaction with both tacrolimus formulations. A higher metabolic baseline capacity appeared to attenuate the extent of induction by SJW. |
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| DOI: | doi:10.1002/cpdd.1364 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1002/cpdd.1364 |
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| | Volltext: https://onlinelibrary.wiley.com/doi/abs/10.1002/cpdd.1364 |
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| | DOI: https://doi.org/10.1002/cpdd.1364 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | drug formulation |
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| | drug-drug interaction |
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| | pharmacogenetics |
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| | St. John's Wort |
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| | tacrolimus |
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| K10plus-PPN: | 1882280881 |
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| Verknüpfungen: | → Zeitschrift |
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Effect of tacrolimus formulation (prolonged-release vs immediate-release) on its susceptibility to drug-drug interactions with St. John's Wort / Gümüs, Katja S. [VerfasserIn]; 04 January 2024 (Online-Ressource)
