ArticleAntimicrobial agents and chemotherapy2009
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed, 68 citations in OpenAlex.
- Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling.Journal of clinical pharmacology · 2022Trial
- Intrapulmonary Pharmacokinetics of Lascufloxacin in Healthy Adult Volunteers.Antimicrobial agents and chemotherapy · 2018Trial
- Moxifloxacin population pharmacokinetics and model-based comparison of efficacy between moxifloxacin and ofloxacin in African patients.Antimicrobial agents and chemotherapy · 2014Trial
- Moxifloxacin population pharmacokinetics in patients with pulmonary tuberculosis and the effect of intermittent high-dose rifapentine.Antimicrobial agents and chemotherapy · 2012Trial
- Impact of rifampicin on P-glycoprotein (ABCB1) expression in M1 and M2 macrophages derived from the THP-1 monocytic cell line or peripheral blood mononuclear cells.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- THP-1-derived polarized macrophages differ by drug transporter transcriptomics, P-glycoprotein activity and rifampicin uptake kinetics.Archives of toxicology · 2026Article
- The role of ABC transporters in the human lung epithelium-insights from and limitations of current in vitro cell models.In vitro models · 2026Review
- Physiologically Based Pharmacokinetic Modeling of Antibiotics in Children: Perspectives on Model-Informed Precision Dosing.Antibiotics (Basel, Switzerland) · 2025Review
- Biomarker-Driven Pharmacokinetics and Efficacy of Polymyxin B in Critically Ill Patients with XDR-GN Pneumonia.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Extrapolation of lung pharmacokinetics of antitubercular drugs from preclinical species to humans using PBPK modelling.The Journal of antimicrobial chemotherapy · 2024Article
- Improved characterization of aminoglycoside penetration into human lung epithelial lining fluid via population pharmacokinetics.Antimicrobial agents and chemotherapy · 2024Article
- Effect of Dexketoprofen on the Disposition Kinetics of Moxifloxacin in Plasma and Lung in Male and Female Rats.Current drug metabolism · 2024Article
- Optimizing Moxifloxacin Dose in MDR-TB Participants with or without Efavirenz Coadministration Using Population Pharmacokinetic Modeling.Antimicrobial agents and chemotherapy · 2023Article
- Clinical Relevance of Rifampicin-Moxifloxacin Interaction in Isoniazid-Resistant/Intolerant Tuberculosis Patients.Antimicrobial agents and chemotherapy · 2022Article
- Prediction of potential drug interactions between repurposed COVID-19 and antitubercular drugs: an integrational approach of drug information software and computational techniques data.Therapeutic advances in drug safety · 2021Article
- Pharmacokinetics and Drug-Drug Interactions of Abacavir and Lamuvudine Co-administered With Antituberculosis Drugs in HIV-Positive Children Treated for Multidrug-Resistant Tuberculosis.Frontiers in pharmacology · 2021Article
- Comparison between Colistin Sulfate Dry Powder and Solution for Pulmonary Delivery.Pharmaceutics · 2020Article
- Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents.Molecules (Basel, Switzerland) · 2019Article
- A Pharmacology Perspective of Simultaneous Tuberculosis and Hepatitis C Treatment.Antimicrobial agents and chemotherapy · 2019Review
- Limited Sampling Strategies Using Linear Regression and the Bayesian Approach for Therapeutic Drug Monitoring of Moxifloxacin in Tuberculosis Patients.Antimicrobial agents and chemotherapy · 2019Article
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Moxifloxacin (MXF) is a fluoroquinolone antibiotic that is effective against respiratory infections. However, the mechanisms of MXF lung diffusion are unknown. Active transport in other tissues has been suggested for several members of the fluoroquinolone family. In this study, transport of MXF was systematically investigated across a Calu-3 lung epithelial cell model. MXF showed polarized transport, with the secretory permeability being twice as high as the absorptive permeability. The secretory permeability was concentration dependent (apparent P(max) = 13.6 x 10(-6) cm x s(-1); apparent K(m) = 147 microM), suggesting saturated transport at concentrations higher than 350 microg/ml. The P-glycoprotein inhibitor PSC-833 inhibited MXF transport in both directions, whereas probenecid, a multidrug resistance-related protein inhibitor, appeared to have no effect in the Calu-3 model. Moreover, rifampin, a known inducer of efflux transport proteins, upregulated the expression of P-glycoprotein in Calu-3 cells and enhanced MXF active transport. In conclusion, this study clearly indicates that MXF is subject to P-glycoprotein-mediated active transport in the Calu-3 model. This P-glycoprotein-dependent secretion may lead to higher MXF epithelial lining fluid concentrations than those in plasma. Furthermore, drug-drug interactions may be expected when MXF is combined with other P-glycoprotein substrates or modulators.
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Registered trials
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