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Linezolid is a member of the oxazolidinone class of medications. [10] Linezolid was discovered in the mid-1990s, and was approved for commercial use in 2000. [16] [17] It is on the World Health Organization's List of Essential Medicines. [18] The World Health Organization classifies linezolid as critically important for human medicine. [19]
It differs from linezolid by replacement of the morpholine oxygen with a sulfur atom. Like linezolid, sutezolid is a bacterial protein synthesis inhibitor . In preclinical studies, sutezolid demonstrated superior antituberculosis activity compared to linezolid.
Skeletal formula of the antibiotic linezolid, highlighting the oxazolidinone pharmacophore (in blue) and desirable structural characteristics (in orange). Created using ACD/ChemSketch 10.0 and Inkscape. Date: 24 June 2009: Source: Own work based on: Brickner SJ (1996). "Oxazolidinone antibacterial agents".
Tedizolid tablets have an oral bioavailability >90%. Tedizolid has higher binding to plasma proteins (80%), longer half-life, and a larger volume of distribution compared to linezolid. It is primarily metabolized by the liver as an inactive sulphate conjugate (phase II reaction), with no metabolism by cytochrome P-450 enzymes.
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The Group A drugs are currently levofloxacin or moxifloxacin, bedaquiline and linezolid, therefore XDR-TB is MDR/RR-TB that is resistant to a fluoroquinolone and at least one of bedaquiline or linezolid (or both). In a study of MDR-TB patients from 2005 to 2008 in various countries, 43.7% had resistance to at least one second-line drug. [28]
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