2008
DOI: 10.1128/aac.00859-08
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In Vitro Activity of TR-700, the Antibacterial Moiety of the Prodrug TR-701, against Linezolid-Resistant Strains

Abstract: TR-701 is the orally active prodrug of TR-700, a novel oxazolidinone that demonstrates four-to eightfoldgreater activity than linezolid (LZD) against Staphylococcus and Enterococcus spp. In this study evaluating the in vitro sensitivity of LZD-resistant isolates, TR-700 demonstrated 8-to 16-fold-greater potency than LZD against all strains tested, including methicillin-resistant Staphylococcus aureus (MRSA), strains of MRSA carrying the mobile cfr methyltransferase gene, and vancomycin-resistant enterococci. T… Show more

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Cited by 165 publications
(139 citation statements)
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References 31 publications
(59 reference statements)
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“…Escherichia coli numbering in parentheses. Model was generated with Chimera 1.10.1 according to K. J. Shaw et al 14, 35…”
Section: Protein Synthesis Inhibitorsmentioning
confidence: 99%
“…Escherichia coli numbering in parentheses. Model was generated with Chimera 1.10.1 according to K. J. Shaw et al 14, 35…”
Section: Protein Synthesis Inhibitorsmentioning
confidence: 99%
“…Tedizolid inhibits the synthesis of bacterial proteins by interacting with the 23S rRNA component of the 50S ribosomal subunit (5). The drug has activity against staphylococci, streptococci, and enterococci, including some strains that have lost susceptibility to vancomycin, daptomycin, and linezolid (Table 1) (6)(7)(8). Additionally, tedizolid has activity against linezolid-resistant Staphylococcus aureus with the cfr multidrug resistance gene mutation (6).…”
Section: Tedizolid Phosphatementioning
confidence: 99%
“…The drug has activity against staphylococci, streptococci, and enterococci, including some strains that have lost susceptibility to vancomycin, daptomycin, and linezolid (Table 1) (6)(7)(8). Additionally, tedizolid has activity against linezolid-resistant Staphylococcus aureus with the cfr multidrug resistance gene mutation (6). Compared to linezolid, tedizolid has been shown to have 4-to 16-fold greater in vitro activity against methicillin-susceptible Staphylococcus aureus (MSSA), MRSA, streptococci, and enterococci (9).…”
Section: Tedizolid Phosphatementioning
confidence: 99%
“…The molecule inhibits translation by binding to the bacterial 23S ribosome initiation complex [100] . Its spectrum covers Grampositive pathogens, including linezolid-resistant S. aureus [101] .…”
Section: Tedizolidmentioning
confidence: 99%