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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].

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