Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid®

  title={Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid{\textregistered}},
  author={Ravi Kanth Bhamidipati and P Venkatesh and Prajakta V. Dravid and Prasad C. Narasimhulu and Sastry Tvrs and Jagattaran Das and Ramesh Mullangi and N. R. Srinivas},
  journal={European Journal of Drug Metabolism and Pharmacokinetics},
SummaryThe aim of this study was to determine the bioavailability of a novel oxazolidinone, DRF-6196, in mice and rats followingintravenous (i.v) and oral dosing and to compare the pharmacokinetics with those obtained following linezolid dosing. Blood samples were drawn at predetermined intervals up to 24 h post-dose after either DRF-6196 or linezolid administration. The concentrations of DRF-6196 and linezolid in various plasma samples were determined by a HPLC method. Following oral… 


Validation of a simple bioanalytical method for the determination of DRF-6196, a novel oxazolidinone, in mouse plasma: application to a single-dose pharmacokinetic study.
An isocratic simple, specific, sensitive and reproducible high performance liquid chromatography (HPLC) method was developed and validated for the estimation of DRF-6196, a novel oxazolidinone in mouse plasma and this method was successfully applied to a pharmacokinetic study of DRFs in mice.
Pharmacokinetic/pharmacodynamic relationships of antimicrobial drugs used in veterinary medicine.
The rise in incidence of antimicrobial resistance, consumer demands and improved understanding of antimicrobial action has encouraged international agencies to review the use of antimicrobial drugs.
The discovery of linezolid, the first oxazolidinone antibacterial agent.
Linezolid possessed a unique mechanism of action in that it inhibited functional 70S initiation complex formation and did not cross-react with existing bacterial resistance, and was selected for continued human clinical evaluation based upon its' superior pharmacokinetic profile.
Oxazolidinones: activity, mode of action, and mechanism of resistance.
Linezolid: a review of its use in the management of serious gram-positive infections.
Linezolid has good activity against gram-positive bacteria, particularly multidrug resistant strains of S. aureus and enterococci, and is poised to play an important role in the management of serious gram- positive infections.
Vancomycin-resistant enterococcal infections.
  • B. Murray
  • Medicine, Biology
    The New England journal of medicine
  • 2000
The emergence of enterococci with resistance to vancomycin, seen predominantly in the species E. faecium, has been followed by an increase in the frequency with which this species is recovered.
The Discovery
  • G. Uhlenbruck
  • Computer Science
    Molecular and Cellular Biochemistry
  • 2005
The genealogical method will connect contemporary struggles over the decolonization of the public space with historical resistance to nation-state integration at the borderlands in Cambedo, a rural community in Trás-os-Montes, with the emphasis reveals otherwise obfuscated historical events and connections.
Epidemiology of nosocomial infections caused by methicillin-resistant Staphylococcus aureus.
A program designed to control a widespread outbreak in a university hospital used three surveillance methods to identify the major institutional reservoir of colonized and infected inpatients and found transient carriage on the hands of hospital personnel appears to be the most important mechanism of serial patient-to-patient transmission.
Linezolid - a review of the first oxazolidinone
  • R. Norrby
  • Biology, Medicine
    Expert opinion on pharmacotherapy
  • 2001
Linezolid is the first of a truly new class of antibiotics, the oxazolidinones, which acts as an inhibitor of bacterial protein synthesis by blocking the formation of the 70S ribosomal initiation complex and is a weak and reversible monoamine oxidase (MAO) inhibitor.