Oxazolidinone for gram-positive infections
IC50: for MAO-A (monoamine oxidase-A), 8.7 uM; for MAO-B, 5.7 uM.
Tedizolid HCl is a reversible, novel oxazolidinone antibiotic. It is the first oxazolidinone to be approved since linezolid in 2000. Tedizolid phosphate is the second commercially available oxazolidinone antibiotic and is the prodrug form of tedizolid with a fixed once-daily dose. As an expanded-spectrum oxazolidinone it has potent activity against a wide range of Gram-positive pathogens [1].
In vitro: In vitro, tedizolid was a reversible inhibitor for both human MAO-A and MAO-B; for MAO-A, the value of IC50 was 8.7 uM, and for MAO-B, the value of IC50 was 5.7 uM. For this two inhibitions, add 46.0 and 2.1 uM of linezolid, respectively would be better [2].
In vivo: It exhibited not only a potent activity against Gram-positive pathogens but also maintained activity against linezolid resistant bacteria. In murine serotonergic model, the number of head twitches was analyzed after tedizolid phosphate was administrated by intraperitoneal injection [2].
Clinical trial: With 200 mg once daily tedizolid would treat the acute bacterial skin and skin structure infections caused by gram-positive bacteria in phase III clinical trials. The treatment effects of tedizolid for ventilator-acquired and health care-associated pneumonia were currently investigated [3].
参考文献:
[1] Chen KH, Huang YT, Liao CH et dl. In Vitro Activities of Tedizolid and Linezolid against Gram-Positive Cocci Associated with Acute Bacterial Skin and Skin Structure Infections and Pneumonia. Antimicrob Agents Chemother. 2015 Oct;59(10):6262-5.
[2] S. Flanagan, K. Bartizal, S. L. Minassian et dl. In Vitro, In Vivo, and Clinical Studies of Tedizolid To Assess the Potential for Peripheral or Central Monoamine Oxidase Interactions. Antimicrob Agents Chemother. 2013 Jul;57(7):3060-6.
[3] Rybak JM, Marx K, Martin CA. Early experience with tedizolid: clinical efficacy, pharmacodynamics, and resistance. Pharmacotherapy. 2014 Nov;34(11):1198-208.
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