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Antimicrobial Agents and Chemotherapy, August 2009, p. 3236-3239, Vol. 53, No. 8
0066-4804/09/$08.00+0     doi:10.1128/AAC.00228-09
Copyright © 2009, American Society for Microbiology. All Rights Reserved.

In Vitro Activity of TR-700, the Active Ingredient of the Antibacterial Prodrug TR-701, a Novel Oxazolidinone Antibacterial Agent {triangledown}

Ronda Schaadt, Debora Sweeney, Dean Shinabarger, and Gary Zurenko*

Micromyx, Kalamazoo, Michigan

Received 18 February 2009/ Returned for modification 9 April 2009/ Accepted 3 June 2009

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.

* Corresponding author. Mailing address: Micromyx, 4717 Campus Drive, Kalamazoo, MI 49008. Phone: (269) 372-3683. Fax: (269) 353-5567. E-mail: gezurenko{at}micromyx.com

{triangledown} Published ahead of print on 15 June 2009.

Antimicrobial Agents and Chemotherapy, August 2009, p. 3236-3239, Vol. 53, No. 8
0066-4804/09/$08.00+0     doi:10.1128/AAC.00228-09
Copyright © 2009, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Locke, J. B., Hilgers, M., Shaw, K. J. (2009). Mutations in Ribosomal Protein L3 Are Associated with Oxazolidinone Resistance in Staphylococci of Clinical Origin. Antimicrob. Agents Chemother. 53: 5275-5278 [Abstract] [Full Text]  


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