ArticleCurrent drug metabolism2022
Pharmacokinetic Study of Vadadustat and High-Resolution Mass Spectrometric Characterization of its Novel Metabolites in Equines for the Purpose of Doping Control.
Article in Current drug metabolism, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
What it found
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Who cites it
3 citing papers in PubMed, 11 citations in OpenAlex.
- Characterization of Novel Metabolites of the HIF Stabilizer JNJ-42041935 in Rats Using LC-HRMS for Doping Control Purposes: A Pilot Study.Drug testing and analysis · 2026Article
- Quantification of osilodrostat in horse urine using LC/ESI-HRMS to establish an elimination profile for doping control.Bioanalysis · 2024Article
- Comparison between standard hematological parameters and blood doping biomarkers in dried blood spots within the athlete population of Swiss Sport Integrity.Frontiers in sports and active living · 2024Article
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Authors and funding
12 authors at 3 institutions in 1 country.
Funding
Abstract
backgroundVadadustat, a hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitor, is a substance which carries a lifetime ban in both horse racing and equestrian competition. A comprehensive metabolic study of vadadustat in horses has not been previously reported.
objectiveMetabolism and elimination profiles of vadadustat in equine plasma and urine were studied for the purpose of doping control.
methodsA nasoesophageal administration of vadadustat (3 g/day for 3 days) was conducted on three thoroughbred mares. Potential metabolites were comprehensively detected by differential analysis of full-scan mass spectral data obtained from both in vitro studies with liver homogenates and post-administration samples using liquid chromatography high-resolution mass spectrometry. The identities of metabolites were further substantiated by product ion scans. Quantification methods were developed and validated for the establishment of the excretion profiles of the total vadadustat (free and conjugates) in plasma and urine.
resultsA total of 23 in vivo and 14 in vitro metabolites (12 in common) were identified after comprehensive analysis. We found that vadadustat was mainly excreted into urine as the parent drug together with some minor conjugated metabolites. The elimination profiles of total vadadustat in post-administration plasma and urine were successfully established by using quantification methods equipped with alkaline hydrolysis for cleavage of conjugates such as methylated vadadustat, vadadustat glucuronide, and vadadustat glucoside.
conclusionBased on our study, for effective control of the misuse or abuse of vadadustat in horses, total vadadustat could successfully be detected for up to two weeks after administration in plasma and urine.
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