ArticleAntimicrobial agents and chemotherapy2010
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 70 citations in OpenAlex.
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- Inherent Fluorescence Demonstrates Immunotropic Properties for Novel Janus Kinase 3 Inhibitors.ACS pharmacology & translational science · 2023Article
- MRSA compendium of epidemiology, transmission, pathophysiology, treatment, and prevention within one health framework.Frontiers in microbiology · 2022Review
- Brief considerations on targeting RNA with small molecules.Faculty reviews · 2022Review
- In vitro antibiotic activity against intraosteoblastic Staphylococcus aureus: a narrative review of the literature.The Journal of antimicrobial chemotherapy · 2021Review
- Excessive lysosomal ion-trapping of hydroxychloroquine and azithromycin.International journal of antimicrobial agents · 2020Article
- Pharmacokinetics of Macrolide Antibiotics and Transport into the Interstitial Fluid: Comparison among Erythromycin, Clarithromycin, and Azithromycin.Antibiotics (Basel, Switzerland) · 2020Article
- Emerging Treatment Options for Infections by Multidrug-Resistant Gram-Positive Microorganisms.Microorganisms · 2020Review
- Radezolid Is More Effective Than Linezolid Against Planktonic Cells and InhibitsFrontiers in microbiology · 2020Article
- Intracellular Penetration and Effects of Antibiotics onAntibiotics (Basel, Switzerland) · 2019Review
- An Expandable Mechanopharmaceutical Device (1): Measuring the Cargo Capacity of Macrophages in a Living Organism.Pharmaceutical research · 2018Article
- Management of drug-resistant tuberculosis in special sub-populations including those with HIV co-infection, pregnancy, diabetes, organ-specific dysfunction, and in the critically ill.Journal of thoracic disease · 2018Review
- Cellular Pharmacokinetics and Intracellular Activity of Gepotidacin against Staphylococcus aureus Isolates with Different Resistance Phenotypes in Models of Cultured Phagocytic Cells.Antimicrobial agents and chemotherapy · 2018Article
- Screening of TB Actives for Activity against Nontuberculous Mycobacteria Delivers High Hit Rates.Frontiers in microbiology · 2017Article
- Transport of Azithromycin into Extravascular Space in Rats.Antimicrobial agents and chemotherapy · 2016Article
- Cellular pharmacokinetics and intracellular activity of the novel peptide deformylase inhibitor GSK1322322 against Staphylococcus aureus laboratory and clinical strains with various resistance phenotypes: studies with human THP-1 monocytes and J774 murine macrophages.Antimicrobial agents and chemotherapy · 2015Article
- Nonclinical and pharmacokinetic assessments to evaluate the potential of tedizolid and linezolid to affect mitochondrial function.Antimicrobial agents and chemotherapy · 2015Article
- Development of a population pharmacokinetic model characterizing the tissue distribution of azithromycin in healthy subjects.Antimicrobial agents and chemotherapy · 2014Article
- An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants.Bioorganic & medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Radezolid (RX-1741) is the first biaryloxazolidinone in clinical development. It shows improved activity, including against linezolid-resistant strains. Radezolid differs from linezolid by the presence of a biaryl spacer and of a heteroaryl side chain, which increases the ionization and hydrophilicity of the molecule at physiological pH and confers to it a dibasic character. The aim of this study was to determine the accumulation and subcellular distribution of radezolid in phagocytic cells and to decipher the underlying mechanisms. In THP-1 human macrophages, J774 mouse macrophages, and human polymorphonuclear neutrophils, radezolid accumulated rapidly and reversibly (half-lives of approximately 6 min and 9 min for uptake and efflux, respectively) to reach, at equilibrium, a cellular concentration 11-fold higher than the extracellular one. This process was concentration and energy independent but pH dependent (accumulation was reduced to 20 to 30% of control values for cells in medium at a pH of <6 or in the presence of monensin, which collapses pH gradients between the extracellular and intracellular compartments). The accumulation at equilibrium was not affected by efflux pump inhibitors (verapamil and gemfibrozil) and was markedly reduced at 4 degrees C but was further increased in medium with low serum content. Subcellular fractionation studies demonstrated a dual subcellular distribution for radezolid, with approximately 60% of the drug colocalizing to the cytosol and approximately 40% to the lysosomes, with no specific association with mitochondria. These observations are compatible with a mechanism of transmembrane diffusion of the free fraction and partial segregation of radezolid in lysosomes by proton trapping, as previously described for macrolides.
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