Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD

WM Bernhardt, MS Wiesener, P Scigalla… - Journal of the …, 2010 - journals.lww.com
The reasons for inadequate production of erythropoietin (EPO) in patients with ESRD are
poorly understood. A better understanding of EPO regulation, namely oxygen-dependent
hydroxylation of the hypoxia-inducible transcription factor (HIF), may enable targeted
pharmacological intervention. Here, we tested the ability of fibrotic kidneys and extrarenal
tissues to produce EPO. In this phase 1 study, we used an orally active prolyl-hydroxylase
inhibitor, FG-2216, to stabilize HIF independent of oxygen availability in 12 hemodialysis …