A physiologically based pharmacokinetic model of ketoconazole and its metabolites as drug-drug interaction perpetrators
The antifungal ketoconazole, which is mainly used for dermal infections and treatment of Cushing’s syndrome, is prone to drug-food interactions (DFIs) and is well known for its strong drug-drug interaction (DDI) potential. Some of ketoconazole’s potent inhibitory activity can be attributed to its me...
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| Hauptverfasser: | , , , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
17 February 2023
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| In: |
Pharmaceutics
Year: 2023, Jahrgang: 15, Heft: 2, Pages: 1-22 |
| ISSN: | 1999-4923 |
| DOI: | 10.3390/pharmaceutics15020679 |
| Online-Zugang: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.3390/pharmaceutics15020679 Verlag, lizenzpflichtig, Volltext: https://www.mdpi.com/1999-4923/15/2/679 
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| Verfasserangaben: | Fatima Zahra Marok, Jan-Georg Wojtyniak, Laura Maria Fuhr, Dominik Selzer, Matthias Schwab, Johanna Weiss, Walter Emil Haefel and Thorsten Lehr |
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| 520 | |a The antifungal ketoconazole, which is mainly used for dermal infections and treatment of Cushing’s syndrome, is prone to drug-food interactions (DFIs) and is well known for its strong drug-drug interaction (DDI) potential. Some of ketoconazole’s potent inhibitory activity can be attributed to its metabolites that predominantly accumulate in the liver. This work aimed to develop a whole-body physiologically based pharmacokinetic (PBPK) model of ketoconazole and its metabolites for fasted and fed states and to investigate the impact of ketoconazole’s metabolites on its DDI potential. ... | ||
| 650 | 4 | |a cytochrome P450 3A4 (CYP3A4) | |
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| 650 | 4 | |a P-glycoprotein (P-gp) | |
| 650 | 4 | |a physiologically based pharmacokinetic (PBPK) modeling | |
| 650 | 4 | |a reversible inhibition | |
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