Abstract
Roxadustat (ROX) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PHI) that exerts erythropoietic, cardioprotective, and metabolic regulatory effects. Approved for the treatment of anemia associated with chronic kidney disease, ROX promotes endogenous erythropoietin production and improves iron homeostasis, providing a non-injectable alternative to conventional erythropoiesis-stimulating agents (ESAs). Its ability to enhance oxygen transport and facilitate muscle recovery has, however, led to its misuse in sports, where it is classified as a banned substance by the World Anti-Doping Agency. This review provides a comprehensive overview of the pharmacological properties of ROX, its approved and investigational clinical applications, and its chemical synthesis strategies. Particular emphasis is placed on the analytical methodologies employed for ROX detection in anti-doping settings. Techniques such as liquid chromatography-tandem mass spectrometry (LC-MS/MS), ultraviolet-visible (UV-Vis) spectroscopy, Fourier-transform infrared spectroscopy (FT-IR), and high-performance thin-layer chromatography (HPTLC) are critically assessed for their efficacy in detecting ROX and its metabolites in biological matrices. Given the increasing incidence of ROX misuse among athletes, ongoing optimization of detection protocols and longitudinal monitoring approaches, are essential to uphold both sports integrity and public health.