Determination of the HCV protease inhibitor telaprevir in plasma and dried blood spot by liquid chromatography-tandem mass spectrometry

Corrien P W G M Verweij-Van Wissen, Marga J A De Graaff-Teulen, Clara T M M De Kanter, Rob E. Aarnoutse*, David M. Burger

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Background: Telaprevir is a protease inhibitor used in the treatment of hepatitis C virus infection. Analytical methods for telaprevir should separate the compound from its R-diastereomer VRT-127394, which is 30-fold less active. The objective of this work was to develop liquid chromatography-tandem mass spectrometer (LC-MS/MS) assays for telaprevir both in plasma and in dried blood spot (DBS), capable of stabilizing the equilibrium and chromatographically separating the 2 epimers. Methods: Human plasma was acidified with formic acid and frozen within 1 hour after collection to stabilize the equilibrium between the 2 telaprevir diastereomers ex vivo in plasma. After protein precipitation, the sample was analyzed with LC-MS/MS. For the DBS assay, sampling paper was impregnated with citric acid solution to achieve stabilization of the epimers on the sampling paper. DBS samples were extracted before LC-MS/MS analysis. LC-MS/MS analysis comprised online solid-phase extraction and separation on a C18 column, with the mass spectrometer operating in TurboIonSpray-negative ionization mode and performing multiple reaction monitoring. Results: The assays were linear over the concentration range of 0.1-10 mg/L in plasma and DBS. Accuracies ranged from 97% to 106% in plasma and from 93% to 99% in DBS. Within- and between-day coefficients of variation were

Original languageEnglish
Pages (from-to)626-633
Number of pages8
JournalTherapeutic Drug Monitoring
Volume37
Issue number5
DOIs
Publication statusPublished - 1 Oct 2015
Externally publishedYes

Keywords

  • Dried blood spot
  • Liquid chromatography-tandem mass spectrometry
  • Plasma
  • Telaprevir

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