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In vivo effects of bempedoic acid on microdosed CYP probe drugs

BackgroundBempedoic acid (BA) is a novel oral cholesterol-lowering drug. So far, in vivo evidence on potential drug-drug interactions via the cytochrome P450 (CYP) enzymes is lacking.MethodsIn a clinical trial, we evaluated the effect of BA on microdosed probe drugs using a limited sampling strategy...

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Hauptverfasser: Stoll, Felicitas E. (VerfasserIn) , Amato, Salvatore (VerfasserIn) , Burhenne, Jürgen (VerfasserIn) , Blank, Antje (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 08 April 2025
In: Frontiers in pharmacology
Year: 2025, Jahrgang: 16, Pages: 1-6
ISSN:1663-9812
DOI:10.3389/fphar.2025.1544956
Online-Zugang:Verlag, kostenfrei, Volltext: https://doi.org/10.3389/fphar.2025.1544956
Verlag, kostenfrei, Volltext: https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2025.1544956/full
Volltext
Verfasserangaben:Felicitas Stoll, Salvatore Amato, Jürgen Burhenne and Antje Blank
Beschreibung
Zusammenfassung:BackgroundBempedoic acid (BA) is a novel oral cholesterol-lowering drug. So far, in vivo evidence on potential drug-drug interactions via the cytochrome P450 (CYP) enzymes is lacking.MethodsIn a clinical trial, we evaluated the effect of BA on microdosed probe drugs using a limited sampling strategy in healthy volunteers. The outcome measures were as follows: 1) the omeprazole AUC0-4h and hydroxylation index (HI) after a 100 µg dose to evaluate CYP2C19 activity, 2) the midazolam AUC2-4h after a 30 µg dose to evaluate CYP3A activity, and 3) the yohimbine AUC0-4h after a 50 µg dose to evaluate CYP2D6 activity. Partial areas under the curve (AUCs) were evaluated at baseline and under BA steady state. The endpoints were the geometric mean ratios (GMRs) with 95% confidence intervals (CI) of the partial AUCs.ResultsIn 15 participants, the AUC0-4h of omeprazole and its HI significantly decreased (GMR: 0.75, 90% CI: 0.66-0.85; change in HI p < 0.0001). There was no change in the AUC2-4h of midazolam (GMR: 1.18, 90% CI: 0.87-1.61) and AUC0-4h of yohimbine (GMR: 0.92, 90% CI: 0.75-1.14).ConclusionIn healthy volunteers, BA was a mild inducer of CYP2C19 and did not affect CYP3A or CYP2D6 activity.
Beschreibung:Veröffentlicht: 08. April 2025
Gesehen am 26.09.2025
Beschreibung:Online Resource
ISSN:1663-9812
DOI:10.3389/fphar.2025.1544956

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