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Linezolid (U-100766 or PNU-100766)

Linezolid  (U-100766 or PNU-100766)

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Product name:Linezolid (U-100766, PNU-100766)

CAS:165800-03-3

MF:C16H20FN3O4

MW:337.35

Description: Linezolid (U-100766, PNU-100766) developed and produced by the US Pharmacia & Upiohn company (which has been acquired by Pfizer) ,is a new type of azole oxazolidinone class of synthetic antibacterial drugs, the FDA on April 18, 2000 approved the drug to market. This product is the first drug in American in 40 years which is approved for the treatment of methicillin-resistant Staphylococcus aureus infection, September 2007 month in China's listed, it belongs to the Medicare B drugs.

Linezolid reached the US market for the treatment of patients with infections caused by serious Gram-positive pathogens, particularly skin and soft tissue infections, communityacquired pneumonia and vancomycin-resistant enterococcal infections. Linezolid is the (S)-enantiomer of an oxazolidin-2-one synthesized in a multistep process from 3,4- difluoronitrobenzene, the key step being the cyclization of a carbamate, using a chiral epoxyester, into an enantiomerically pure oxazolidin-2-one. Linezolid can be considered as the first of a new class of antibacterial agents known as oxazolidinones, its mechanism of action being related to the inhibition of early ribosomal protein synthesis without directly inhibiting DNA or RNA synthesis. In vitro studies demonstrated that linezolid was effective, at potency levels similar to vancomycin, against staphylococcal, streptococcal and pneumococcal infections (MIC values in the range of 0.5 to 2 g/ml), enterococcal species including VRE and VSE (MIC values about 4 g/ml), but also other vancomycin-resistant bacteria. Linezolid is rapidly absorbed orally, its bioavailability is nearly complete at 250 mg dose giving a Cmax to MIC ratio sufficient to have pathogenic strain eradication in the clinical setting. It is considered that this new promising agent may offer new options for therapy of multi-drug infections.

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