Skin and soft tissue concentrations of tedizolid (formerly torezolid), a novel oxazolidinone, following a single oral dose in healthy volunteers.

International Journal of Antimicrobial Agents
Martina SahreHartmut Derendorf

Abstract

Plasma concentrations of antimicrobial drugs have long been used to correlate exposure with effect, yet one cannot always assume that unbound plasma and tissue concentrations are similar. Knowledge about unbound tissue concentrations is important in the development of antimicrobial drugs, since most infections are localised in tissues. Therefore, a clinical microdialysis study was conducted to evaluate the distribution of tedizolid (TR-700), the active moiety of the antimicrobial prodrug tedizolid phosphate (TR-701), into interstitial fluid (ISF) of subcutaneous adipose and skeletal muscle tissues following a single oral 600 mg dose of tedizolid phosphate in fasting conditions. Twelve healthy adult subjects were enrolled. Two microdialysis probes were implanted into the thigh of each subject, one into the vastus medialis muscle and one into subcutaneous adipose tissue. Probes were calibrated using retrodialysis. Dialysate samples were collected every 20 min for 12h following a single oral dose of 600 mg tedizolid phosphate, and blood samples were drawn over 24h. Unbound tedizolid levels in plasma were similar to those in muscle and adipose tissue. The ratios of unbound (free) AUC in tissues over unbound AUC in plasma (fAUC(tiss...Continue Reading

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References

Mar 10, 1973·British Medical Journal·G D ChisholmL P Garrod
Mar 1, 1983·The Journal of Antimicrobial Chemotherapy·D J MerrikinG N Rolinson
Apr 1, 1993·Journal of Pharmacological and Toxicological Methods·E J EisenbergK C Cundy
May 27, 2005·Antimicrobial Agents and Chemotherapy·Pejman DehghanyarChristian Joukhadar
Apr 27, 2007·Pharmaceutical Research·Chandra S ChaurasiaHelen Yeo
Nov 15, 2007·The Journal of Antimicrobial Chemotherapy·Christiane ThallingerChristian Joukhadar
Dec 22, 2007·Scandinavian Journal of Infectious Diseases·Lars B StolleCharlotte Kloft
Apr 15, 2009·Antimicrobial Agents and Chemotherapy·April BarbourHartmut Derendorf
Aug 12, 2010·JAMA : the Journal of the American Medical Association·Alexander J KallenUNKNOWN Active Bacterial Core surveillance (ABCs) MRSA Investigators of the Emerging Infections Program
Nov 16, 2011·Antimicrobial Agents and Chemotherapy·Anthony M NicasioGeorge L Drusano

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Citations

Dec 18, 2013·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·William O'RiordanPhilippe Prokocimer
Apr 17, 2013·Drug Design, Development and Therapy·Olatz UrbinaSantiago Grau
Feb 20, 2014·Journal of Pharmaceutical Sciences·Jatinder Kaur MukkerHartmut Derendorf
Sep 30, 2015·Drugs in R&D·Gerard KennedyShellie Bertolami
Oct 1, 2014·Pharmacotherapy·Jeffrey M RybakCraig A Martin
Mar 17, 2016·Expert Opinion on Drug Metabolism & Toxicology·Dario CattaneoMichael Neely
Oct 3, 2015·Journal of the American Podiatric Medical Association·Seth T HousmanDavid P Nicolau
Jul 24, 2013·Expert Opinion on Pharmacotherapy·Jeffrey M RybakMichael J Rybak
Feb 25, 2015·Infectious Diseases and Therapy·Jeffrey M Rybak, Karrine Roberts
Apr 19, 2016·Journal of Medicinal Chemistry·Renee BouleyMayland Chang
Jan 25, 2017·Current Opinion in Infectious Diseases·Mordechai Grupper, David P Nicolau
Apr 6, 2017·Journal of Chemotherapy·Silvano EspositoUNKNOWN Italian Society of Infectious and Tropical Diseases
Oct 25, 2017·Clinical Pharmacokinetics·Claire RogerLaurent Muller
Sep 20, 2017·Antimicrobial Agents and Chemotherapy·Barbara A Brown-Elliott, Richard J Wallace
Apr 5, 2013·Clinical Microbiology Reviews·Daniel GonzalezHartmut Derendorf
Mar 24, 2017·Journal of Clinical Microbiology·Barbara A Brown-Elliott, Richard J Wallace
Aug 20, 2014·Antimicrobial Agents and Chemotherapy·S FlanaganP Prokocimer
Apr 2, 2014·American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists·Jamie J KisgenLindsey M Childs
May 26, 2020·Expert Review of Clinical Pharmacology·Alberto A Carena, Martin E Stryjewski
Jul 14, 2018·Infectious Diseases and Therapy·Sergey ShlyapnikovMark H Wilcox

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