Determination of epacadostat, a novel IDO1 inhibitor in mouse plasma by LC–MS/MS and its application to a pharmacokinetic study in mice

Vinay Dhiman, Kalpesh Kumar Giri, S. Suresh P., Mohd Zainuddin, Sriram Rajagopal, Ramesh Mullangi*

*Corresponding author for this work

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

A sensitive, specific and rapid LC-ESI-MS/MS method has been developed and validated for the quantification of epacadostat in mouse plasma using tolbutamide as an internal standard (IS) as per regulatory guidelines. Sample preparation was accomplished through a protein precipitation. Chromatographic separation was performed on an Atlantis dC18 column using a binary gradient using mobile phase A (acetonitrile) and B (0.2% formic acid in water) at a flow rate of 0.90 mL/min. Elution of epacadostat and IS occurred at ~2.41 and 2.51 min, respectively. The total chromatographic run time was 3.2 min. A linear response function was established in the concentration range of 1.07–533 ng/mL. The intra- and inter-day accuracy and precision were in the ranges of 1.81–12.9 and 3.80–11.1%, respectively. This novel method has been applied to a pharmacokinetic study in mice.

Original languageEnglish
Article numbere3794
Number of pages8
JournalBiomedical Chromatography
Volume31
Issue number2
DOIs
Publication statusPublished - Feb 2017
Externally publishedYes

Keywords

  • epacadostat
  • LC–MS/MS
  • method validation
  • mouse plasma
  • pharmacokinetics

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