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

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 (r² = 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.