Review of Eravacycline, a Novel Fluorocycline Antibacterial Agent

@article{Zhanel2016ReviewOE,
  title={Review of Eravacycline, a Novel Fluorocycline Antibacterial Agent},
  author={George G. Zhanel and Doris Man Chi Cheung and Heather J. Adam and Sheryl A. Zelenitsky and Alyssa R. Golden and Frank Schweizer and Bala Kishan Gorityala and P. Lagac{\'e}-Wiens and Andrew Walkty and Alfred S. Gin and Daryl J. Hoban and James A. Karlowsky},
  journal={Drugs},
  year={2016},
  volume={76},
  pages={567-588}
}
Eravacycline is an investigational, synthetic fluorocycline antibacterial agent that is structurally similar to tigecycline with two modifications to the D-ring of its tetracycline core: a fluorine atom replaces the dimethylamine moiety at C-7 and a pyrrolidinoacetamido group replaces the 2-tertiary-butyl glycylamido at C-9. [...] Key Result Oral bioavailability of eravacycline is estimated at 28 % (range 26–32 %) and a single oral dose of 200 mg achieves a maximum plasma concentration (Cmax) and area under the…Expand
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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. Expand
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Clinical trials of complicated intra-abdominal infection, acute pelvic infection, complicated skin and soft-structure infection, community-acquired pneumonia and complicated urinary tract infections demonstrated that ertapenem has equivalent efficacy and safety compared with ceftriaxone and piperacillin/tazobactam. Expand
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Eravacycline (TP-434) Is Efficacious in Animal Models of Infection
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Eravacycline was efficacious in mouse septicemia models, demonstrating 50% protective dose values of ≤1 mg/kg of body weight once a day against Staphylococcus aureus, and was active in multiple murine models of infection against clinically important Gram-positive and Gram-negative pathogens. Expand
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Eravacycline has a broad-spectrum activity toward pathogens involved in complicated urinary tract (cUTIs) and intra-abdominal infections (cIAIs), including extended-spectrums beta-lactamase and carbapenem-resistant Enterobacteriaceae, methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci. Expand
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This and the accompanying report (DOI: 10.1021/jm201467r ) describe the design, synthesis, and evaluation of a new generation of tetracycline antibacterial agents,Expand
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