NCIt definition : An orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI),
with potential anti-anemic activity. Upon administration, roxadustat binds to and
inhibits HIF-PHI, an enzyme responsible for the degradation of transcription factors
in the HIF family under normal oxygen conditions. This prevents HIF breakdown and
promotes HIF activity. Increased HIF activity leads to an increase in endogenous erythropoietin
production, thereby enhancing erythropoiesis. It also reduces the expression of the
peptide hormone hepcidin, improves iron availability, and boosts hemoglobin (Hb) levels.
HIF regulates the expression of genes in response to reduced oxygen levels, including
genes required for erythropoiesis and iron metabolism.;