Single- and multiple-dose pharmacokinetics and absolute bioavailability of tedizolid.
Bottom Line: Treatment-related adverse events occurred in 41% of subjects.Most adverse events were related to infusion site and became more frequent with multiple dosing.These results from a population of healthy volunteers support once/day dosing of tedizolid phosphate 200 mg with both the oral and IV formulations, without the need for dose adjustment when switching administration routes.
Affiliation: Cubist, San Diego, California.Show MeSH
Related in: MedlinePlus
Mentions: Following IV administration of tedizolid phosphate 200 mg, plasma tedizolid phosphate concentrations reached a plateau by the first time point (15 min postdose), decreased rapidly at the end of the infusion, and generally fell below the LLOQ by 2 hours after the start of the infusion (Figure2). The mean (SD) Cmax, AUC0–∞, and t1/2 of tedizolid phosphate following IV administration of 200 mg over 1 hour were 2.1 (0.3) μg/ml, 1.8 (0.2) μg × hour/ml, and 11.8 (3.0) minute, respectively. After oral administration of tedizolid phosphate 200 mg, all tedizolid phosphate plasma measurements were below the LLOQ. Urine levels of tedizolid phosphate were generally below the LLOQ and, in the few subjects with detectable concentrations, accounted for less than 0.005% of the total administered dose. Because of the very low tedizolid phosphate exposure, analyses focused on the PK of the active moiety tedizolid.