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tedizolid
Tedizolid Phosphate (formerly torezolid phosphate, TR-701), is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals), and is marketed, under the trade name Sivextro, for the treatment of acute bacterial skin and skin structure infections (also known as complicated skin and skin-structure infections (cSSSIs)).
Tedizolid has been approved by the U.S Food and Drug Administration on June 20, 2014, for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by certain susceptible bacteria, including Staphylococcus aureus (including methicillin-resistant strains (MRSA) and methicillin-susceptible strains), various Streptococcus species (S. pyogenes, S. agalactiae, and S. anginosus Group including S. anginosus, S. intermedius, and S. constellatus), and Enterococcus faecalis.〔("Sivextro Prescribing info" ). Lexington, MA: Cubist.Updated March 2015.〕 Tedizolid is a second-generation oxazolidinone that is 4-to-16-fold more potent against staphylococci and enterococci compared to linezolid.〔("Tedizolid (TR-701): a new oxazolidinone with enhanced potency" ). Accessed 2015-03-16.〕 The recommended dosage for treatment is 200 mg once daily for a total duration of six days, either orally (with or without food) or through an intravenous injection (if patient is older than 18 years old).〔
==Mechanism of Action==
Tedizolid phosphate is a prodrug activated by plasma or intestinal phosphatases to tedizolid following administration of the drug either orally or intravenously.〔 The prodrug tedizolid is called "TR-701", while the active moiety is called "TR-700".〔("In Vitro Activity of TR-700, the Active Ingredient of the Antibacterial Prodrug TR-701, a Novel Oxazolidinone Antibacterial Agent" ). Accessed 2015-03-16.〕 Once activated, tedizolid exerts its bacteriostatic microbial activity through inhibition of protein synthesis by binding to the 50S ribosomal subunit of the bacteria.〔
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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