HIF prolyl-hydroxylase inhibitor

HIF prolyl-hydroxylase inhibitor
Drug class
Roxadustat, the first marketed HIF prolyl-hydroxylase inhibitor
Class identifiers
ATC codeB03X
Mechanism of actionEnzyme inhibitor
Biological targetHIF prolyl-hydroxylase
Legal status
In Wikidata
Not to be confused with Factor Inhibiting HIF Asparaginyl Hydroxylase Inhibitors.

Hypoxia-inducible factor prolyl hydroxylase inhibitors (HIF-PHIs) are a novel class of oral medications developed for the treatment of anemia in chronic kidney disease (CKD). These drugs work by inhibiting hypoxia-inducible factor-proline dioxygenase (HIF prolyl-hydroxylase), which are responsible for the degradation of hypoxia-inducible factor (HIF) under normal oxygen conditions.[1] By stabilizing HIF, these inhibitors mimic the body's natural response to hypoxia, leading to increased endogenous erythropoietin production and improved iron metabolism.[2] HIF-PHIs have shown efficacy in correcting and maintaining hemoglobin levels in both dialysis-dependent and non-dialysis-dependent CKD patients, offering an alternative to traditional erythropoiesis-stimulating agents (ESAs).[1][3]

  1. ^ a b Stoumpos S, Crowe K, Sarafidis P, Barratt J, Bolignano D, Del Vecchio L, et al. (September 2024). "Hypoxia-inducible factor prolyl hydroxylase inhibitors for anaemia in chronic kidney disease: a clinical practice document by the European Renal Best Practice board of the European Renal Association". Nephrology, Dialysis, Transplantation. 39 (10): 1710–1730. doi:10.1093/ndt/gfae075. PMC 11427073. PMID 38573822.
  2. ^ Cite error: The named reference Haase_2021 was invoked but never defined (see the help page).
  3. ^ Li J, Haase VH, Hao CM (January 2023). "Updates on Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors in the Treatment of Renal Anemia". Kidney Diseases. 9 (1). Basel, Switzerland: 1–11. doi:10.1159/000527835. PMC 9900466. PMID 36756084.