Linezolid, the first oxazolidinone antibacterial agent

作者：Karen L. Leach, Steven J. Brickner, Mark C. Noe, Paul F. Miller · 发表于：Annals of the New York Academy of Sciences · 年份：2011 · DOI：10.1111/j.1749-6632.2011.05962.x · 被引用次数：196 · 研究领域：Antimicrobial Resistance in Staphylococcus、Antibiotic Resistance in Bacteria、Bacterial Identification and Susceptibility Testing

Linezolid (Zyvox) is the first member of an entirely new class of antibiotics to reach the market in over 35 years; it was approved for use in 2000. A member of the oxazolidinone class of antibiotics, linezolid is highly effective for the treatment of serious Gram-positive infections and has activity that compares favorably with vancomycin for most clinically relevant pathogens. Zyvox is approved for use against serious Gram-positive infections, including those caused by Streptococcus pneumoniae, and the very challenging methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium organisms. Zyvox inhibits bacterial protein synthesis by binding to 23S rRNA in the catalytic site of the 50S ribosome. It can be administered both orally and intravenously and has good tissue distribution. Recent results have demonstrated that oxazolidinone analogs related to linezolid are effective in treating pulmonary tuberculosis caused by resistant Mycobacterium tuberculosis in animal infection models and suggest additional new therapeutic applications for these antibiotics.