title: In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
abstract: TR-701 is the prodrug of the microbiologically active molecule TR-700, a novel orally and intravenously administered oxazolidinone antibacterial agent. The in vitro activity of TR-700 was evaluated against 1,063 bacterial clinical isolates including staphylococci, enterococci, streptococci, Moraxella catarrhalis, Haemophilus influenzae, and a variety of anaerobic bacterial species. The test strains were recent (2005 to 2008) clinical isolates from diverse U.S. (80%) and non-U.S. (20%) sites. MIC assays were conducted using reference broth microdilution and agar dilution methods with the principal comparators linezolid and vancomycin. TR-700 was four- to eightfold more potent than linezolid against staphylococci and generally fourfold more potent against enterococci and streptococci. TR-700 was less active against M. catarrhalis and H. influenzae but was twofold more active than linezolid. Against anaerobic species, the activity of TR-700 was equivalent to or up to fourfold higher than that of linezolid. These results indicate that TR-700 is a promising new oxazolidinone antibacterial agent with greater in vitro potency than linezolid against clinically important gram-positive bacteria.
authors.affiliation: Micromyx, 4717 Campus Drive, Kalamazoo, MI 49008, USA.
authors.forename: Ronda
authors.initials: R
authors.lastname: Schaadt
authors.forename: Debora
authors.initials: D
authors.lastname: Sweeney
authors.forename: Dean
authors.initials: D
authors.lastname: Shinabarger
authors.forename: Gary
authors.initials: G
authors.lastname: Zurenko
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D016983:Enterococcus / Q000187:drug effects; D006193:Haemophilus influenzae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D001936:Moraxella catarrhalis / Q000187:drug effects; D023303:Oxazolidinones / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones