Pharmacokinetics, Safety, and Tolerability of Tedizolid Phosphate in Elderly Subjects

Clin Pharmacol Drug Dev. 2018 Sep;7(7):788-794. doi: 10.1002/cpdd.426. Epub 2018 Jan 10.

Abstract

Tedizolid phosphate is approved for the treatment of acute bacterial skin and skin structure infections in adults. We evaluated the pharmacokinetics of tedizolid in elderly subjects to guide dosing recommendations. In an open-label phase 1 study (ClinicalTrials.gov identifier NCT01496677), 14 elderly (≥65 years) and 14 younger control (18-45 years) subjects each received a single oral dose of tedizolid phosphate 200 mg. Blood samples were collected before dose and more than 72 hours after dose. The pharmacokinetic parameters of tedizolid after a single dose were similar in both age groups. Geometric mean ratios (elderly/younger controls) and corresponding 90% confidence intervals were maximum observed plasma concentration (Cmax ), 1.091 (0.917-1.297); AUC from time 0 extrapolated to infinity (AUC0-∞ ), 1.132 (0.954-1.343). Tedizolid plasma exposure was similar in elderly and younger control subjects. The findings indicated that after intravenous or oral administration of tedizolid phosphate 200 mg once daily, no dose adjustment was warranted in elderly subjects to achieve therapeutic levels.

Keywords: ABSSSI; SSTI; antibacterial; oxazolidinone; population pharmacokinetics; tedizolid.

Publication types

  • Clinical Trial, Phase I
  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intravenous
  • Administration, Oral
  • Adult
  • Aged
  • Area Under Curve
  • Biological Availability
  • Drug Administration Schedule
  • Female
  • Humans
  • Male
  • Organophosphates / administration & dosage*
  • Organophosphates / adverse effects
  • Organophosphates / pharmacokinetics*
  • Oxazoles / administration & dosage*
  • Oxazoles / adverse effects
  • Oxazoles / pharmacokinetics*

Substances

  • Organophosphates
  • Oxazoles
  • tedizolid phosphate

Associated data

  • ClinicalTrials.gov/NCT01496677