ArticleClinical pharmacokinetics2025
Improving Understanding of Fexofenadine Pharmacokinetics to Assess Pgp Phenotypic Activity in Older Adult Patients Using Population Pharmacokinetic Modeling.
Article in Clinical pharmacokinetics, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT03477331 (Antithrombotics' Therapeutic Optimization in Hospitalized Patients Using Physiologically- and Population-based Pharmacokinetic Modeling), which is not on this map. Cited by 3 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Antithrombotics' Therapeutic Optimization in Hospitalized Patients Using Physiologically- and Population-based Pharmacokinetic Modeling
Who cites it
3 citing papers in PubMed.
- Potential Links Between Aging, Mitochondrial Dysfunction, and Drug Transporter Function-Molecular Mechanisms and Pharmacokinetic Implications.International journal of molecular sciences · 2026Review
- Recent Advances in Oral Drug Delivery Systems for BCS III Drugs.Current issues in molecular biology · 2026Review
- Changed expression of placental transporters and disrupted epigenetic patterns in a rat model of schizophrenia.Frontiers in pharmacology · 2025Article
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectiveFexofenadine is commonly used as a probe substrate to assess P-glycoprotein (Pgp) activity. While its use in healthy volunteers is well documented, data in older adult and polymorbid patients are lacking. Age- and disease-related physiological changes are expected to affect the pharmacokinetics of fexofenadine. This study aims to investigate the pharmacokinetics of fexofenadine in hospitalized older adult patients as a potential marker of Pgp activity, using data from the OptimAT study (ClinicalTrials.gov identifier: NCT03477331).
methodsPopulation pharmacokinetic (popPK) modeling was conducted using data from 449 hospitalized patients with a median age of 71 years (range: 25-97) and 10 healthy volunteers (median age: 23 years, range: 20-36). Fexofenadine plasma concentrations were analyzed using a refined two-compartment model with sequential zero/first-order absorption, while investigating the impact of covariates such as age, renal function, and Pgp inhibitors on fexofenadine pharmacokinetics.
resultsAge, renal insufficiency, and Pgp inhibitors significantly influenced fexofenadine exposure. Renal function was a key factor, with AUC
conclusionClinicians should consider the risk of Pgp substrate accumulation in older adults, particularly those with advanced renal impairment. We propose typical values stratified by age and renal function to assist in interpreting Pgp phenotyping using fexofenadine exposure, thereby supporting drug optimization in this population. Further studies are needed to explore underlying mechanisms, such as reduced Pgp activity or expression.
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