Prolyl hydroxylase inhibitors: a breakthrough in the therapy of anemia associated with chronic diseases

AA Joharapurkar, VB Pandya, VJ Patel… - Journal of medicinal …, 2018 - ACS Publications
AA Joharapurkar, VB Pandya, VJ Patel, RC Desai, MR Jain
Journal of medicinal chemistry, 2018ACS Publications
Chronic kidney disease, cancer, chronic inflammatory disorders, nutritional, and genetic
deficiency can cause anemia. Hypoxia causes induction of hypoxia-inducible factor (HIF),
which stimulates erythropoietin (EPO) synthesis. Prolyl hydroxylase domain (PHD) enzyme
inhibition can stabilize hypoxia-inducible factor (HIF). HIF stabilization also decreases
hepcidin, a hormone of hepatic origin, which regulates iron homeostasis. PHD inhibitors
represent a novel pharmacological treatment of anemia associated with chronic diseases …
Chronic kidney disease, cancer, chronic inflammatory disorders, nutritional, and genetic deficiency can cause anemia. Hypoxia causes induction of hypoxia-inducible factor (HIF), which stimulates erythropoietin (EPO) synthesis. Prolyl hydroxylase domain (PHD) enzyme inhibition can stabilize hypoxia-inducible factor (HIF). HIF stabilization also decreases hepcidin, a hormone of hepatic origin, which regulates iron homeostasis. PHD inhibitors represent a novel pharmacological treatment of anemia associated with chronic diseases. Many orally active PHD inhibitors like roxadustat, molidustat, vadadustat, and desidustat are in late phase clinical trials. This review discusses the role of PHD inhibitors in the treatment of anemia associated with chronic diseases.
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