ArticleAntimicrobial agents and chemotherapy2010
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
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 19 papers.
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Who cites it
19 citing papers in PubMed, 49 citations in OpenAlex.
- In Vitro Activities of Oxazolidinone Antibiotics Alone and in Combination with C-TEMPO against Methicillin-ResistantAntibiotics (Basel, Switzerland) · 2023Article
- Side-by-Side Profiling of Oxazolidinones to Estimate the Therapeutic Window against Mycobacterial Infections.Antimicrobial agents and chemotherapy · 2023Article
- 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
- Investigational and Experimental Drugs for Community-Acquired Pneumonia: the Current Evidence.Journal of experimental pharmacology · 2020Review
- Radezolid Is More Effective Than Linezolid Against Planktonic Cells and InhibitsFrontiers in microbiology · 2020Article
- Article
- Staphylococcus aureus vs. Osteoblast: Relationship and Consequences in Osteomyelitis.Frontiers in cellular and infection microbiology · 2015Review
- An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants.Bioorganic & medicinal chemistry · 2014Article
- Leishmania panamensis infection and antimonial drugs modulate expression of macrophage drug transporters and metabolizing enzymes: impact on intracellular parasite survival.The Journal of antimicrobial chemotherapy · 2014Article
- Investigational antimicrobial agents of 2013.Clinical microbiology reviews · 2013Review
- Pharmacodynamic evaluation of the intracellular activity of antibiotics towards Pseudomonas aeruginosa PAO1 in a model of THP-1 human monocytes.Antimicrobial agents and chemotherapy · 2013Article
- New antibiotic agents in the pipeline and how they can help overcome microbial resistance.Virulence · 2013Review
- Influence of the protein kinase C activator phorbol myristate acetate on the intracellular activity of antibiotics against hemin- and menadione-auxotrophic small-colony variant mutants of Staphylococcus aureus and their wild-type parental strain in human THP-1 cells.Antimicrobial agents and chemotherapy · 2012Article
- Newer antibacterials in therapy and clinical trials.North American journal of medical sciences · 2012Article
- Pharmacodynamic evaluation of the activity of antibiotics against hemin- and menadione-dependent small-colony variants of Staphylococcus aureus in models of extracellular (broth) and intracellular (THP-1 monocytes) infections.Antimicrobial agents and chemotherapy · 2012Article
- Evidence of significant synergism between antibiotics and the antipsychotic, antimicrobial drug flupenthixol.European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology · 2012Article
- Linezolid Resistance in Staphylococci.Pharmaceuticals (Basel, Switzerland) · 2010Review
- Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.Antimicrobial agents and chemotherapy · 2010Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Radezolid is a novel biaryloxazolidinone in clinical development which shows improved activity, including against linezolid-resistant strains. In a companion paper (29), we showed that radezolid accumulates about 11-fold in phagocytic cells, with approximately 60% of the drug localized in the cytosol and approximately 40% in the lysosomes of the cells. The present study examines its activity against (i) bacteria infecting human THP-1 macrophages and located in different subcellular compartments (Listeria monocytogenes, cytosol; Legionella pneumophila, vacuoles; Staphylococcus aureus and Staphylococcus epidermidis, mainly phagolysosomal), (ii) strains of S. aureus with clinically relevant mechanisms of resistance, and (iii) isogenic linezolid-susceptible and -resistant S. aureus strains infecting a series of phagocytic and nonphagocytic cells. Radezolid accumulated to similar levels ( approximately 10-fold) in all cell types (human keratinocytes, endothelial cells, bronchial epithelial cells, osteoblasts, macrophages, and rat embryo fibroblasts). At equivalent weight concentrations, radezolid proved consistently 10-fold more potent than linezolid in all these models, irrespective of the bacterial species and resistance phenotype or of the cell type infected. This results from its higher intrinsic activity and higher cellular accumulation. Time kill curves showed that radezolid's activity was more rapid than that of linezolid both in broth and in infected macrophages. These data suggest the potential interest of radezolid for recurrent or persistent infections where intracellular foci play a determinant role.
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