Evidence map›Paper›PMID 22584101›Full record

ArticleInternational journal of antimicrobial agents2012

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

Martina Sahre, Sreedharan Sabarinath, Maria Grant, Christoph Seubert, Carisa Deanda, Philippe Prokocimer, Hartmut Derendorf

Registry-linked trialAbstract read
In one paragraph

Article in International journal of antimicrobial agents, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT00666601 (An Open Label, Single Dose, Microdialysis and Pharmacokinetic Study of TR-701 in Normal Healthy Adults), which is not on this map. Cited by 29 papers, 2 of them syntheses that pooled it.

0numbers the graph read from it
0cells of the map it votes in
29citing papers in PubMed, 2 pooled it
3.5field-weighted citation impact, top 7% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

NCT00666601 phase1completednot on this map

An Open Label, Single Dose, Microdialysis and Pharmacokinetic Study of TR-701 in Normal Healthy Adults

TypeinterventionalSponsorTrius Therapeutics LLC, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)Ran2008 to 2008Enrolled15ConditionsHealthyArmsTR-700 (active moiety), TR-701 (pro-drug)
3 · Its place in the literature

Who cites it

29 citing papers in PubMed, 2 syntheses or guidelines pooled it, 60 citations in OpenAlex.

  1. Pooled it
  2. Pooled it
  3. Trial
  4. Article
  5. Observational
  6. Effect of the human endotoxin challenge on tedizolid tissue penetration.British journal of clinical pharmacology · 2023
    Article
  7. Review
  8. Importance and Reality of TDM for Antibiotics Not Covered by Insurance in Japan.International journal of environmental research and public health · 2022
    Review
  9. Article
  10. Antibiotics in Necrotizing Soft Tissue Infections.Antibiotics (Basel, Switzerland) · 2021
    Review
  11. Article
  12. Article
  13. Review
  14. Article
  15. Antimicrobial agents and chemotherapy · 2017
    Article
  16. Journal of clinical microbiology · 2017
    Article
  17. Review
  18. Article
  19. Article
  20. Tedizolid Phosphate: a Next-Generation Oxazolidinone.Infectious diseases and therapy · 2015
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors at 3 institutions in 1 country.

Martina SahreUniversity of Florida, College of Pharmacy, Department of Pharmaceutics, 1600 SW Archer Road, JHMHC, PO Box 100494, Gainesville, FL 32610, USA.
Sreedharan Sabarinath
Maria Grant
Christoph Seubert
Carisa Deanda
Philippe Prokocimer
Hartmut Derendorf
University of Florida · USArcturus Therapeutics (United States) · USFlorida College · US

Funding

WHITE MATTER AND COGNITION IN PARKINSON'S DISEASEM01RR000082 · NCRR · UNIVERSITY OF FLORIDA · PI FOOTE, KELLY D · 1985 to 2009
$29.7M
NCRR NIH HHS M01 RR0000082NCRR NIH HHS M01 RR000082
6 · The paper itself

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(tissue)/fAUC(plasma)) were 1.1 ± 0.2 and 1.2 ± 0.2 for adipose and muscle tissue, respectively. The median half-life was 8.1, 9.2 and 9.6h for plasma, adipose tissue and muscle tissue, respectively. Mean protein binding was 87.2 ± 1.8%. The study drug was very well tolerated. The results of this study show that tedizolid distributes well into ISF of adipose and muscle tissues. Unbound levels of tedizolid in plasma, adipose tissue and muscle tissue were well correlated. Free plasma levels are indicative of unbound levels in the ISF of muscle and adipose tissues.

Indexed as

Administration, OralAdolescentAdultAnti-Bacterial AgentsArea Under CurveExtracellular FluidFemaleHealthy VolunteersHumansMaleMiddle AgedMuscle, SkeletalOxazolidinonesSubcutaneous FatTetrazolesTime FactorsAnti-Bacterial AgentsOxazolidinonestedizolidTetrazoles

Identifiers

PMID22584101
PMCPMC3789129
OpenAlexW1981107394

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.