Trial reportBritish journal of clinical pharmacology2011
Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects.
Trial report in British journal of clinical pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed, 34 citations in OpenAlex.
- Serum 4β-hydroxycholesterol increases during fluconazole treatment.European journal of clinical pharmacology · 2021Trial
- Pharmacokinetics and Drug Interactions.Pharmaceutics · 2026Article
- Comprehensive Management of HIV With Multiple Opportunistic Infections: A Case Report.Clinical case reports · 2025Article
- 1β-Hydroxydeoxycholic acid as an endogenous biomarker in human plasma for assessment of drug-drug interaction with moderate CYP3A inhibitor.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Physiologically Based Pharmacokinetic Modeling of Tofacitinib: Predicting Drug Exposure and Optimizing Dosage in Special Populations and Drug-Drug Interaction Scenarios.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Population-based screening to detect benzodiazepine drug-drug-drug interaction signals associated with unintentional traumatic injury.Scientific reports · 2022Article
- Effect of fluconazole on the pharmacokinetics of fuzuloparib: an open-label, crossover study in Chinese healthy male volunteers.Cancer chemotherapy and pharmacology · 2022Article
- Evaluation of 1β-Hydroxylation of Deoxycholic Acid as a Non-Invasive Urinary Biomarker of CYP3A Activity in the Assessment of Inhibition-Based Drug-Drug Interaction in Healthy Volunteers.Journal of personalized medicine · 2021Article
- Effect of CYP3A inhibitors on the pharmacokinetics of pevonedistat in patients with advanced solid tumours.British journal of clinical pharmacology · 2019Article
- Article
- Overactive bladder, differential diagnosis, and clinical utility of fesoterodine.International journal of general medicine · 2012Article
- Clinical pharmacology of functional disorders of the urogenital system.British journal of clinical pharmacology · 2011Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
what is already known about this subjectAvailable data suggest that fesoterodine dosage should not exceed 4 mg once daily when taken concomitantly with potent CYP3A4 inhibitors, such as ketoconazole. Currently, no information is available on whether dose adjustment is necessary when fesoterodine is administered with a moderate CYP3A4 inhibitor. WHAT THIS STUDY ADDS: This study shows that adjustment of fesoterodine dose is not warranted when co-administered with a moderate CYP3A4 inhibitor.
aimsTo assess the effects of fluconazole, a moderate CYP3A4 inhibitor, on the pharmacokinetics (PK) and safety/tolerability of fesoterodine.
methodsIn this open-label, randomized, two-way crossover study, 28 healthy subjects (18-55 years) received single doses of fesoterodine 8 mg alone or with fluconazole 200 mg. PK endpoints, including the area under the plasma concentration-time curve from 0 to infinity (AUC(0,∞)), maximum plasma concentration (C(max) ), time to C(max) (t(max) ), and half-life (t(1/2) ), were assessed for 5-hydroxymethyl tolterodine (5-HMT), the active moiety of fesoterodine.
resultsConcomitant administration of fesoterodine with fluconazole increased AUC(0,∞) and C(max) of 5-HMT by approximately 27% and 19%, respectively, with corresponding 90% confidence intervals of (18%, 36%) and (11%, 28%). There was no apparent effect of fluconazole on 5-HMT t(max) or t(½) . Fesoterodine was generally well tolerated regardless of fluconazole co-administration, with no reports of death, serious adverse events (AEs) or severe AEs. Following co-administration of fesoterodine with fluconazole, 13 subjects (48%) experienced a total of 40 AEs; following administration of fesoterodine alone, six subjects (22%) experienced a total of 19 AEs. The majority of AEs were of mild intensity. There were no clinically significant changes in laboratory or physical examination parameters.
conclusionFesoterodine 8 mg single dose was well tolerated when administered alone or with fluconazole. Based on the observed increase in 5-HMT exposures being within the inherent variability of 5-HMT pharmacokinetics, adjustment of fesoterodine dose is not warranted when co-administered with a moderate CYP3A4 inhibitor provided they are not also inhibitors of transporters.
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