Small-molecule inhibitors of HIF-PHD2: a valid strategy to renal anemia treatment in clinical therapy?

MedChemComm Pub Date: 2016-05-25 DOI: 10.1039/C6MD00240D

Abstract

Patients with chronic kidney diseases (CKD) always suffer from anemia with severe impacts on their quality of life. Erythropoiesis-stimulating agents (ESAs) are the main drugs in clinical therapy. However, the side effects and high price of ESAs scare off many patients. Small-molecule inhibitors of hypoxia inducing factor proline hydroxylase domain 2 (HIF-PHD2) solves these problems elegantly in clinical therapy. The strategy of inhibiting HIF-PHD2 to improve renal anemia is via the upregulating of hypoxia inducing factor-2α (HIF-2α) for increased expression of downstream genes such as erythropoietin (EPO) and vascular endothelial growth factor (VEGF). This review introduces the function of small-molecule HIF-PHD2 inhibitors for improving renal anemia and summarizes the small-molecule inhibitors of HIF-PHD2 currently in clinical studies.

Graphical abstract: Small-molecule inhibitors of HIF-PHD2: a valid strategy to renal anemia treatment in clinical therapy
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