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Pilot study characterizes metabolites of HIF prolyl hydroxylase inhibitor in rats, enabling enhanced doping detection methods.
Hypoxia‐inducible factor prolyl hydroxylase inhibitors (HIF‐PHIs) stimulate erythropoiesis and enhance performance, and were banned by the World Anti‐Doping Agency in the year 2011. JNJ‐42041935, a potent and selective PHD inhibitor, was administered orally to Sprague–Dawley rats, and its metabolites were tentatively characterized using liquid chromatography‐high‐resolution mass spectrometry (LC‐HRMS) in positive and negative ionization modes. Eleven metabolites were identified, with Phase I reactions including monohydroxylation, dechlorination, and decarboxylation, and Phase II reactions comprising methylation, glucuronidation, sulfation, glycine, and taurine conjugation. These results provide insights into JNJ‐42041935 biotransformation and support the development of analytical methods for HIF‐PHI detection in anti‐doping control. Future studies will continue to identify and characterize the valuable metabolites of JNJ‐42041935, with a view to providing a more comprehensive understanding of its in vivo metabolic profile and developing improved detection methods.
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Hou et al. (2026) studied this question.
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