Eravacycline, also known as TP-434, a novel antibiotics. 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. 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.
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Xiao, Xiao-Yi; Hunt, Diana K.; Zhou, Jingye; Clark, Roger B.; Dunwoody, Nick; Fyfe, Corey; Grossman, Trudy H.; O'Brien, William J.; Plamondon, Louis; Ronn, Magnus; Sun, Cuixiang; Zhang, Wu-Yan; Sutcliffe, Joyce A. Fluorocyclines. 1. 7-Fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: A Potent, Broad Spectrum Antibacterial Agent. Journal of Medicinal Chemistry. Volume 55. Issue 2. Pages 597-605. Journal; Online Computer File. (2012).
Zhang, Wu-Yan; Lafrance, Danny; Ronn, Magnus P. Semisynthesis procedure for the preparation of C7-fluoro substituted tetracycline. Assignee Tetraphase Pharmaceuticals, Inc., USA. WO 2016065290. (2016).
