First detection/quantification of roxadustat in hair with a new liquid chromatography with tandem mass spectrometry method: Application to a treated patient

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Alvarez, Jean Claude | Etting, Isabelle | Juillard, Laurent | Massy, Ziad | Larabi, Islam Amine

Edité par CCSD ; Elsevier -

International audience. Roxadustat is an oral inhibitor of hypoxia-inducible factor prolyl hydroxylase which increases erythropoiesis. It can therefore be used as a doping agent. No data are available on how to measure roxadustat in hair and on the concentration found in treated patients. The aim of this study was to develop a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the quantification of roxadustat in hair and to apply it to a chronically treated patient. After decontamination with dichloromethane, testosterone-D3 used as an internal standard and phosphate buffer pH 5.0 were added to 20 mg of hair and incubated for 10 min at 95 °C. Four ml of dichloromethane were used for extraction and reconstituted into the mobile phase, 10 µL were injected into the chromatographic system. The method was linear in the range 0.5–200 pg/mg, accurate and precise (evaluated at 3 levels) and was successfully applied to measure roxadustat in a brown-haired patient treated pharmacologically with 100–120 mg 3 days a week. Results were stable between 41 and 57 pg/mg in the 6 proximal 1 cm segments. This first method describing the measurement of roxadustat in hair appears to be suitable for the quantification of this compound in clinical or doping control cases.

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