-2%
Erenzo 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.
Erenzo is indicated for the treatment of symptomatic anemia in adult patients with chronic kidney disease (CKD).
Roxadustat, the active ingredient in Erenzo, is an orally bioavailable HIF-PH inhibitor (HIF-PHI) with anti-anemic properties. By inhibiting HIF-PH enzymes responsible for HIF degradation under normoxic conditions, roxadustat stabilizes HIF transcription factors and enhances their activity.
Activation of the HIF pathway results in:
Increased endogenous erythropoietin production
Enhanced erythropoiesis
Reduced hepcidin expression
Improved iron absorption, transport, and utilization
Increased hemoglobin (Hb) levels
Clinical studies have demonstrated that roxadustat induces coordinated erythropoiesis, increasing red blood cell counts while maintaining EPO levels within or near physiological ranges. This effect is observed in both dialysis-dependent and non-dialysis CKD patients, including those with inflammation, without the need for supplemental intravenous iron.
Additionally, roxadustat improves iron metabolism by increasing serum transferrin levels, enhancing intestinal iron absorption, and mobilizing stored iron. A significant reduction in cholesterol levels from baseline has also been observed, irrespective of concurrent statin or lipid-lowering therapy.