ArticlePharmaceutical research2004
Transport characteristics of fexofenadine in the Caco-2 cell model.
Article in Pharmaceutical research, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 129 citations in OpenAlex.
- A modified grapefruit juice eliminates two compound classes as major mediators of the grapefruit juice-fexofenadine interaction: an in vitro-in vivo "connect".Journal of clinical pharmacology · 2013Trial
- Ampicillin Is a Substrate of Organic Anion Transporters 3.Biopharmaceutics & drug disposition · 2026Article
- Improving the Accuracy of Permeability Data to Gain Predictive Power: Assessing Sources of Variability in Assays Using Cell Monolayers.Membranes · 2024Review
- Predicting disruptions to drug pharmacokinetics and the risk of adverse drug reactions in non-alcoholic steatohepatitis patients.Acta pharmaceutica Sinica. B · 2023Review
- Development of a Hierarchical Support Vector Regression-Based In Silico Model for Caco-2 Permeability.Pharmaceutics · 2021Article
- Effect ofPharmaceutics · 2020Article
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- The influence of piperine on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers.European journal of clinical pharmacology · 2017Article
- Antitubercular Agent Delamanid and Metabolites as Substrates and Inhibitors of ABC and Solute Carrier Transporters.Antimicrobial agents and chemotherapy · 2016Article
- The Blood-Brain Barrier Permeability of Lignans and Malabaricones from the Seeds of Myristica fragrans in the MDCK-pHaMDR Cell Monolayer Model.Molecules (Basel, Switzerland) · 2016Article
- To Apply Microdosing or Not? Recommendations to Single Out Compounds with Non-Linear Pharmacokinetics.Clinical pharmacokinetics · 2016Article
- Membrane Assays to Characterize Interaction of Drugs with ABCB1.The Journal of membrane biology · 2015Article
- Carbopol-incorporated thermoreversible gel for intranasal drug delivery.Molecules (Basel, Switzerland) · 2015Article
- A primary fish gill cell culture model to assess pharmaceutical uptake and efflux: evidence for passive and facilitated transport.Aquatic toxicology (Amsterdam, Netherlands) · 2015Article
- Quantitative assessment of intestinal first-pass metabolism of oral drugs using portal-vein cannulated rats.Pharmaceutical research · 2015Article
- In vitro-in situ permeability and dissolution of fexofenadine with kinetic modeling in the presence of sodium dodecyl sulfate.European journal of drug metabolism and pharmacokinetics · 2012Article
- Fruit juice inhibition of uptake transport: a new type of food-drug interaction.British journal of clinical pharmacology · 2010Review
- Coexistence of passive and carrier-mediated processes in drug transport.Nature reviews. Drug discovery · 2010Review
- Evaluation of in vivo P-glycoprotein phenotyping probes: a need for validation.Clinical pharmacokinetics · 2010Review
- Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.Antimicrobial agents and chemotherapy · 2010Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the membrane transport mechanisms of fexofenadine in the Caco-2 model.
methodsTransport studies were performed in Caco-2 cell monolayers 21-25 days after seeding. The apparent permeability (Papp) of fexofenadine was determined in the concentration range 10-1000 microM in the basolateral-to-apical (b-a) and 50-1000 microM in the apical-to-basolateral (a-b) direction. The concentration-dependent effects of various inhibitors of P-glycoprotein (P-gp) (GF120918, ketoconazole, verapamil, erythromycin), multidrug resistant associated protein (MRP) (indomethacin, probenecid), and organic anion transporting polypeptide (OATP) (rifamycin SV) on the bidirectional transport of 150 microM fexofenadine were also examined.
resultsFexofenadine displayed polarized transport, with the Pappb-a being 28- to 85-fold higher than the Papp(a-b). The Papp(a-b) was independent of the concentration applied, whereas Pappb-a decreased with increasing concentration (Vmax = 5.21 nmol cm(-2)s(-1) and K(M) = 150 microM), suggesting saturation of an apical efflux transporter. All four P-gp inhibitors had a strong, concentration-dependent effect on the Papp of fexofenadine in both directions, with GF 120918 being the most specific among them. The IC50 of verapamil was 8.44 microM on the P-gp-mediated secretion of fexofenadine. The inhibitors of OATP or MRP appeared not to affect the Papp(a-b) of fexofenadine in the Caco-2 model.
conclusionsThis study clearly indicates that P-gp was the main transport protein of fexofenadine in the Caco-2 model. Even though P-gp was completely inhibited, fexofenadine was predicted to have a low fraction dose absorbed in humans due to poor intestinal permeability, and low passive diffusion seems to be the major absorption mechanism.
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