Abstract
Eravacycline (TP-434 or 7-fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline) is a novel fluorocycline that was evaluated for antimicrobial activity against panels of recently isolated aerobic and anaerobic Gram-negative and Gram-positive bacteria. Eravacycline showed potent broad-spectrum activity against 90% of the isolates (MIC90) in each panel at concentrations ranging from ≤0.008 to 2 μg/ml for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia (MIC90 values of 32 μg/ml for both organisms). The antibacterial activity of eravacycline was minimally affected by expression of tetracycline-specific efflux and ribosomal protection mechanisms in clinical isolates. Furthermore, eravacycline was active against multidrug-resistant bacteria, including those expressing extended-spectrum β-lactamases and mechanisms conferring resistance to other classes of antibiotics, including carbapenem resistance. Eravacycline has the potential to be a promising new intravenous (i.v.)/oral antibiotic for the empirical treatment of complicated hospital/health care infections and moderate-to-severe community-acquired infections.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP-Binding Cassette Transporters / genetics
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ATP-Binding Cassette Transporters / metabolism
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Community-Acquired Infections / drug therapy
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Community-Acquired Infections / microbiology
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Cross Infection / drug therapy
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Cross Infection / microbiology
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Drug Resistance, Multiple, Bacterial / drug effects*
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Drug Resistance, Multiple, Bacterial / genetics
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Gene Expression
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Gram-Negative Bacteria / drug effects*
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Gram-Negative Bacteria / genetics
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Gram-Negative Bacteria / isolation & purification
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Gram-Negative Bacterial Infections / drug therapy
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Gram-Negative Bacterial Infections / microbiology
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / genetics
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Gram-Positive Bacteria / isolation & purification
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Gram-Positive Bacterial Infections / drug therapy
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Gram-Positive Bacterial Infections / microbiology
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Humans
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Microbial Sensitivity Tests
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Tetracyclines / chemistry
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Tetracyclines / pharmacology*
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beta-Lactamases / genetics
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beta-Lactamases / metabolism
Substances
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ATP-Binding Cassette Transporters
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Anti-Bacterial Agents
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Tetracyclines
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eravacycline
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beta-Lactamases