Daprodustat is a small molecule drug primarily developed for the treatment of anemia associated with chronic kidney disease (CKD). It functions as a hypoxia-inducible factor prolyl hydroxylase inhibitor, which enhances erythropoiesis by mimicking the physiological response to low oxygen levels. This mechanism stimulates the production of erythropoietin, a hormone that promotes red blood cell formation. Daprodustat is characterized by its ability to increase hemoglobin levels without the need for traditional erythropoiesis-stimulating agents, potentially offering a safer alternative with a lower risk of hypertension and cardiovascular events. The compound is administered orally and has been evaluated in clinical trials for its efficacy and safety profile. Its pharmacokinetics involve absorption, metabolism, and excretion that are influenced by various factors, including renal function. Overall, daprodustat represents a novel approach in managing anemia in CKD patients, aiming to improve quality of life and reduce the need for blood transfusions.

Daprodustat

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Inhibitor of HIF-prolyl hydroxylase isozymes PHD1, PHD2 and PHD3 with Ki in nanomolar range. The compound mimics the binding of N-oxalylglycine, chelates catalytic iron and prevents substrate entry into catalytic site. Inhibition of PHD enzymes leads to stabilization of hypoxia-induced factors HIF1α and HIF2α, followed by the production of erythropoietin (EPO).

GSK 1278863

Applications Daprodustat is a novel HIF (Hypoxia inducible factor)-prolyl hydroxylase inhibitor.
References Olson, E., et al.: Vasc. Med., 19, 473 (2014);


Daprodustat (GSK1278863) is a HIF-prolyl hydroxylase inhibitor.

CAS 960539-70-2: Daprodustat

GSK 1278863

Ref: 3D-BG166670

Daprodustat

Ref: TR-D193368

Daprodustat

Ref: TM-T3197