-5%
Roxadustat is indicated for the treatment of symptomatic anemia in adult patients with chronic kidney disease (CKD), including both dialysis-dependent and non–dialysis-dependent patients.
- Children: Roxadustat is not indicated for pediatric use.
- Hepatic impairment: Not recommended in patients with severe liver dysfunction.
Roxadustat is a first-in-class, orally administered hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. It stimulates erythropoiesis by increasing endogenous erythropoietin (EPO) production, improving iron utilization, and counteracting inflammation-mediated suppression of hemoglobin synthesis through downregulation of hepcidin.
Roxadustat is an orally bioavailable HIF-PH inhibitor with potent anti-anemic activity. By reversibly inhibiting HIF-PH enzymes, it prevents the degradation of hypoxia-inducible factor (HIF-α) under normal oxygen conditions, thereby enhancing HIF transcriptional activity.
Activation of the HIF pathway leads to:
- Increased endogenous erythropoietin production
- Enhanced red blood cell formation
- Reduced hepcidin expression
- Improved iron absorption, transport, and mobilization
Roxadustat promotes coordinated erythropoiesis while maintaining plasma EPO levels within or near physiological ranges. It has demonstrated effectiveness across multiple CKD subpopulations, including patients with inflammation, without the routine need for intravenous iron supplementation.
In patients with CKD-associated anemia, Roxadustat dose-dependently increases hemoglobin levels, reduces hepcidin concentrations, and improves iron metabolism by increasing serum transferrin, intestinal iron absorption, and release of stored iron. Additionally, Roxadustat has been shown to significantly reduce total cholesterol levels, regardless of concomitant statin or lipid-lowering therapy.