The DOI matches its Crossref record; 40 of the 40 references it cites were found in a registry or an index.
Tedizolid for the Management of Human Infections: In Vitro Characteristics
Abstract
The emerging antibiotic resistance of Gram-positive pathogens represents a significant challenge to the management of human infections. The novel oxazolidinone tedizolid demonstrates antimicrobial activity across a broad range of Gram-positive pathogens and greater potency than linezolid against wild-type and drug-resistant pathogens, including linezolid-resistant Staphylococcus aureus strains possessing mutations in chromosomal genes encoding 23S rRNA or ribosomal proteins L3 or L4. Strains harboring such mutations are also selected for much less frequently with tedizolid than with linezolid. In addition, tedizolid has a significant potency advantage over linezolid-resistant strains carrying the horizontally transferable cfr gene. Methylation of A2503 of 23S rRNA by the Cfr methyltransferase confers resistance to linezolid (and a variety of other 50S ribosomal subunit-targeted antibiotics) but not to tedizolid because of structural differences in A-ring C5 substituents between the 2 drugs. The greater potency and improved resistance profile of tedizolid provides the microbiologic basis for considering this molecule as an alternative to linezolid for the treatment of serious infections caused by Gram-positive pathogens.
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“Importantly, carriage of cfr does not appear to confer resistance to the recently FDA-approved oxazolidinone tedizolid (67).”
From Mechanisms of Antibiotic Resistance (2016) · cites this paper as [67]
Citations
Cites
Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically
Ferraro, M. J. (2000) · Cited by 16,875
Clinical and Laboratory Standards Institute
Gressner, A. M., & Arndt, T. (2019) · Springer Reference Medizin · doi:10.1007/978-3-662-48986-4_300416 · Cited by 5,092
Linezolid resistance in a clinical isolate of Staphylococcus aureus
Tsiodras, S., Gold, H. S., Sakoulas, G., Eliopoulos, G. M., Wennersten, C. B., Venkataraman, L., Moellering, R. C., & Ferraro, M. J. (2001) · The Lancet · doi:10.1016/s0140-6736(01)05410-1 · Cited by 1,034
Infections due to vancomycin-resistant Enterococcus faecium resistant to linezolid
Gonzales, R. D., Schreckenberger, P. C., Graham, M. B., Kelkar, S., DenBesten, K., & Quinn, J. P. (2001) · The Lancet · doi:10.1016/s0140-6736(00)04376-2 · Cited by 542
Development of in vitro susceptibility testing criteria and quality control parameters
Novick, W. J. (1989) · Clinical Microbiology Newsletter · doi:10.1016/0196-4399(89)90068-8 · Cited by 409
Resistance to Linezolid Caused by Modifications at Its Binding Site on the Ribosome
Long, K. S., & Vester, B. (2011) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.05702-11 · Cited by 377
Tedizolid Phosphate vs Linezolid for Treatment of Acute Bacterial Skin and Skin Structure Infections
Prokocimer, P., Anda, C. S. D., Fang, E., Mehra, P., & Das, A. (2013) · JAMA · doi:10.1001/jama.2013.241 · Cited by 362
Schwarz, Š., Werckenthin, C., & Kehrenberg, C. (2000) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.44.9.2530-2533.2000 · Cited by 342
Toh, S., Xiong, L., Arias, C. A., Villegas, M. V., Lolans, K., Quinn, J., & Mankin, A. S. (2007) · Molecular Microbiology · doi:10.1111/j.1365-2958.2007.05744.x · Cited by 338
The emerging problem of linezolid-resistant Staphylococcus
Gu, B., Kelesidis, T., Tsiodras, S., Hindler, J. A., & Humphries, R. M. (2012) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dks354 · Cited by 332
Research works printed but not linked: 2
- Fang, 2013, Efficacy and safety results from the ESTABLISH 2 ABSSSI study comparing IV and oral tedizolid phosphate and linezolid
- ClinTrials.gov, Pulmonary disposition of TR-700 following once-daily oral 200 mg
Cited by
Sorted by citations
Mechanisms of Antibiotic Resistance
Munita, J. M., & Arias, C. A. (2016) · Microbiology Spectrum · doi:10.1128/microbiolspec.vmbf-0016-2015 · Cited by 2,782
“Carriage of cfr does not appear to confer resistance to the recently FDA-approved oxazolidinone tedizolid (67).”
BackgroundAntibiotic resistance in Staphylococcus aureus. Current status and future prospects
Foster, T. J. (2017) · FEMS Microbiology Reviews · doi:10.1093/femsre/fux007 · Cited by 930
“The newer oxazolidinone tedilozid is active against strains expressing Cfr resistance because its binding is not occluded by methylation of A2503 (Locke et al. 2014).”
BackgroundInfluentialWang, Y., Lv, Y., Cai, J., Schwarz, Š., Cui, L., Hu, Z., Zhang, R., Li, J., Zhao, Q., He, T., et al. (2015) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dkv116 · Cited by 546
Antibiotic Resistance and the MRSA Problem
Vestergaard, M. R., Frees, D., & Ingmer, H. (2019) · Microbiology Spectrum · doi:10.1128/microbiolspec.gpp3-0057-2018 · Cited by 540
“Fortunately, tedizolid, a second-generation oxazolidinone, retains activity against strains carrying cfr (168).”
BackgroundMechanisms of antibiotic resistance
Munita, J. M., & Arias, C. A. (2016) · Virulence Mechanisms of Bacterial Pathogens · doi:10.1128/9781555819286.ch17 · Cited by 421
Metadata
- Authors
- Locke, J. B., Zurenko, G. E., Shaw, K. J., & Bartizal, K.
- Affiliations
- Cubist Pharmaceuticals (United States) (US)
- Venue
- Clinical Infectious Diseases
- Publisher
- Oxford University Press (OUP)
- Published
- 2014-01-01
- Volume
- 58
- Issue
- suppl_1
- Pages
- S35-S42
- ISSN
- 1058-4838 (ISSN-L)
- 1537-6591
- OpenAlex
- W2017411933
- Cited by
- 101
- References
- 40
- Citations by year
- 2026: 1 · 2025: 3 · 2024: 3 · 2023: 3 · 2022: 4 · 2021: 9 · 2020: 3 · 2019: 10 · 2018: 9 · 2017: 13 · 2016: 22 · 2015: 13 · 2014: 8
- FWCI
- 1.86
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Clinical Infectious Diseases (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antimicrobial Resistance in Staphylococcus
- Health Sciences › Medicine › Microbiology (medical) › Antibiotic Resistance in Bacteria
- Health Sciences › Medicine › Infectious Diseases › Antibiotic Use and Resistance
- Keywords
- tedizolid, oxazolidinones, linezolid resistance, Gram-positive bacterial infections, Staphylococcus aureus, 23S rRNA mutations, cfr gene, antimicrobial susceptibility, in vitro antimicrobial activity
- MeSH terms
- Linezolid, Acetamides, Ribosomal Protein L3, Anti-Bacterial Agents, Humans, Oxazoles, Organophosphates, Ribosomal Proteins, RNA, Ribosomal, 23S, tRNA Methyltransferases, Staphylococcal Infections, Staphylococcus aureus, Point Mutation, Gene Transfer, Horizontal, Oxazolidinones, Drug Resistance, Bacterial
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