ABSTRACT
Linezolid (previously U-100766) was the first in a new class of completely synthetic antimicrobial agents, the oxazolidinones. It was approved for clinical use in the USA in April 2000 after a priority review by the US Food and Drug Administration (FDA). Initial indications for therapy included vancomycin-resistant Enterococcus faecium infection, nosocomial pneumonia, and complicated skin and skin structure infection (Meka and Gold, 2004). The E I du Pont de Nemours company developed the early oxazolidinones in the late 1980s; however, toxicity prevented further development (Slee et al., 1987). Linezolid, an (S)-5-acetamidomethyl-2 derivative, was later developed by Upjohn (later Pharmacia and Upjohn) and was released for clinical use after phase I clinical trials demonstrated no major toxic effects (Brickner et al., 1996; Diekema and Jones, 2001). The full name of linezolid is (S)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide; its empirical formula is C16H20FN3O4, it has a molecular weight of 337.35, and the chemical structure is shown in Figure 73.1. Pfizer now markets linezolid under the trade name Zyvox. It is available as an intravenous (IV) suspension for injection, and as tablets and a liquid suspension for oral administration. Chemical structure of linezolid. https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig73_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/>
