Previous Article | Next Article ![]()
Antimicrobial Agents and Chemotherapy, December 2008, p. 4442-4447, Vol. 52, No. 12
0066-4804/08/$08.00+0 doi:10.1128/AAC.00859-08
Copyright © 2008, American Society for Microbiology. All Rights Reserved.

Trius Therapeutics, Inc., San Diego, California,1 Micromyx, Kalamazoo, Michigan,2 Eurofins Medinet, Inc., Herndon, Virginia3
Received 27 June 2008/ Returned for modification 8 September 2008/ Accepted 28 September 2008
TR-701 is the orally active prodrug of TR-700, a novel oxazolidinone that demonstrates four- to eightfold-greater activity than linezolid (LZD) against Staphylococcus and Enterococcus spp. In this study evaluating the in vitro sensitivity of LZD-resistant isolates, TR-700 demonstrated 8- to 16-fold-greater potency than LZD against all strains tested, including methicillin-resistant Staphylococcus aureus (MRSA), strains of MRSA carrying the mobile cfr methyltransferase gene, and vancomycin-resistant enterococci. The MIC90 for TR-700 against LZD-resistant S. aureus was 2 µg/ml, demonstrating the utility of TR-700 against LZD-resistant strains. A model of TR-700 binding to 23S rRNA suggests that the increased potency of TR-700 is due to additional target site interactions and that TR-700 binding is less reliant on target residues associated with resistance to LZD.
Published ahead of print on 6 October 2008.
This article has been cited by other articles:
Copyright © 2009 by the American Society for Microbiology. For an alternate route to Journals.ASM.org, visit: http://intl-journals.asm.org | More Info»