Liquid chromatography-tandem mass spectrometric assay for the quantification of galunisertib in human plasma and the application in a pre-clinical study

M M Tibben, S Huijberts, W Li, A H Schinkel, A Gebretensae, H Rosing, J H Beijnen

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Galunisertib is an anti-cancer drug currently evaluated in phase I and II clinical trials. This study describes the development and validation of a bioanalytical assay to quantify galunisertib in human plasma using HPLC-MS/MS. Stable isotope labelled galunisertib was added as internal standard and the analyte and internal standard were extracted from the matrix by protein precipitation using acetonitrile-methanol (50:50, v/v). Final extracts were injected onto a C18 column, gradient elution was applied for chromatographic separation and detection was performed using a triple quadrupole mass spectrometer operating in the positive ion mode. The assay was linear over the range 0.05-10 ng/mL, with acceptable accuracy (bias ranging from -6.1 to 3.1%) and precision (below 5.7% C.V.) values. The applicability of the assay was demonstrated in a pharmacokinetic experiment in mice.

Original languageEnglish
Pages (from-to)169-175
Number of pages7
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume173
DOIs
Publication statusPublished - 5 Sept 2019

Keywords

  • Galunisertb
  • LC–MS/MS
  • quantification
  • assay
  • human plasma
  • mouse plasma

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