达普司他 (Jesduvroq)

概览

Daprodustat is a small-molecule hypoxia-inducible factor prolyl hydroxylase inhibitor used for the treatment of anemia in patients with chronic kidney disease.

作用机制

Chronic kidney disease (CKD) is associated with several complications, including anemia. The development of anemia in patients with CKD is mostly due to the kidneys' inability to produce a sufficient amount of erythropoietin (EPO). Daprodustat is a potent reversible inhibitor of hypoxia-inducible factor (HIF)-prolyl hydroxylase (PH) 1, PH2 and PH3, with an IC in the low nM range. By inhibiting HIF-PHDs, daprodustat promotes the stabilization and nuclear accumulation of HIF-1α and HIF-2α transcription factors. HIF-α translocates to the nucleus and binds to hypoxia response elements (HREs) on DNA to promote the production of EPO as well as proteins involved in iron uptake, mobilization, and transport. Ultimately, erythropoiesis is increased, iron transport is upregulated, and circulating Hb levels are elevated.

适应症

用于治疗由慢性肾脏病（CKD）导致的肾性贫血，包括透析和非透析CKD患者。

• Anemia