Pharmacokinetics of tedizolid following oral administration: single and multiple dose, effect of food, and comparison of two solid forms of the prodrug.
Bottom Line: The relative bioavailability of TPD to the free acid tedizolid phosphate was determined to bridge the results of these and other studies to the solid form of the prodrug selected for further development.Tedizolid half-life values were approximately 2-fold greater compared with linezolid.TPD administration with food delayed tedizolid absorption and reduced Cmax relative to the fasted state but did not alter AUC.
Affiliation: Trius Therapeutics, San Diego, California.Show MeSH
Mentions: In Study TR701-108, oral administration of equivalent tedizolid doses from either TPD or tedizolid phosphate resulted in a nearly identical concentration profile (Figure 5). Peak (Cmax) and overall (AUC0–t and AUC0–∞) exposures to tedizolid for both formulations differed by less than 5% with the geometric mean ratios and associated 90% CI falling entirely within the 80–125% bioequivalence range (Table 5). Results were consistent at the individual level with no outliers observed for AUC0–∞ or Cmax (Figure 6). Compared with TPD, median time to maximum concentration (Tmax) was similar (2.5–3.0 hrs) and the mean half-life (t½) was the same for both drug products (11.4 hrs; Table 5).