Determination of nifeviroc, a novel CCR5 antagonist: application to a pharmacokinetic study

J Pharm Biomed Anal. 2011 Nov 1;56(3):637-40. doi: 10.1016/j.jpba.2011.06.027. Epub 2011 Jul 5.

Abstract

Nifeviroc is a novel CCR5 antagonist used for the treatment of HIV type-1 infection. A LC-ESI-MS/MS method for the determination of nifeviroc in human plasma was developed and validated. The calibration curve (r(2)=0.9993) of nifeviroc was established at the range of 1.924-2935 μg L(-1). The intra- and inter-day precisions (RSD%) were all less than 7%, and the accuracies at three concentration levels were all within 100 ± 5%. This validated method was then successfully applied to a pharmacokinetic study in health Chinese volunteers.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • CCR5 Receptor Antagonists*
  • Calibration
  • Carbamates / blood*
  • Carbamates / pharmacokinetics*
  • Chromatography, Liquid / methods*
  • Humans
  • Middle Aged
  • Placebos
  • Pyrrolidines / blood*
  • Pyrrolidines / pharmacokinetics*
  • Reference Standards
  • Reproducibility of Results
  • Spectrometry, Mass, Electrospray Ionization / methods*
  • Young Adult

Substances

  • CCR5 Receptor Antagonists
  • Carbamates
  • Placebos
  • Pyrrolidines
  • nifeviroc