A validated bioanalytical HPLC method for pharmacokinetic evaluation of 2-deoxyglucose in human plasma

Murugesan K. Gounder, Hongxia Lin, Mark Stein, Susan Goodin, Joseph R. Bertino, Ah Ng Tony Kong, Robert S. Dipaola

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


2-Deoxyglucose (2-DG), an analog of glucose, is widely used to interfere with glycolysis in tumor cells and studied as a therapeutic approach in clinical trials. To evaluate the pharmacokinetics of 2-DG, we describe the development and validation of a sensitive HPLC fluorescent method for the quantitation of 2-DG in plasma. Plasma samples were deproteinized with methanol and the supernatant was dried at 45°C. The residues were dissolved in methanolic sodium acetate-boric acid solution. 2-DG and other monosaccharides were derivatized to 2-aminobenzoic acid derivatives in a single step in the presence of sodium cyanoborohydride at 80°C for 45min. The analytes were separated on a YMC ODS C 18 reversed-phase column using gradient elution. The excitation and emission wavelengths were set at 360 and 425nm. The 2-DG calibration curves were linear over the range of 0.63-300μg/mL with a limit of detection of 0.5μg/mL. The assay provided satisfactory intra-day and inter-day precision with RSD less than 9.8%, and the accuracy ranged from 86.8 to 110.0%. The HPLC method is reproducible and suitable for the quantitation of 2-DG in plasma. The method was successfully applied to characterize the pharmacokinetics profile of 2-DG in patients with advanced solid tumors.

Original languageEnglish
Pages (from-to)650-654
Number of pages5
JournalBiomedical Chromatography
Issue number5
StatePublished - May 2012


  • 2-deoxyglucose
  • Fluorescence derivatization
  • HPLC
  • Pharmacokinetics

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Molecular Biology
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry


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