title: Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens.
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.
authors: Tetraphase Pharmaceuticals, Inc., Watertown, Massachusetts, USA.
authors: J A
authors: JA
authors: Sutcliffe
authors: W
authors: W
authors: O'Brien
authors: C
authors: C
authors: Fyfe
authors: T H
authors: TH
authors: Grossman
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000235:genetics / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D017714:Community-Acquired Infections / Q000188:drug therapy / Q000382:microbiology; D003428:Cross Infection / Q000188:drug therapy / Q000382:microbiology; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects* / Q000235:genetics; D015870:Gene Expression; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000235:genetics / Q000302:isolation & purification; D016905:Gram-Negative Bacterial Infections / Q000188:drug therapy / Q000382:microbiology; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000235:genetics / Q000302:isolation & purification; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy / Q000382:microbiology; D006801:Humans; D008826:Microbial Sensitivity Tests; D013754:Tetracyclines / Q000737:chemistry / Q000494:pharmacology*; D001618:beta-Lactamases / Q000235:genetics / Q000378:metabolism
chemical_list: D018528:ATP-Binding Cassette Transporters; D000900:Anti-Bacterial Agents; D013754:Tetracyclines; C571179:eravacycline; D001618:beta-Lactamases
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