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Daprodustat is a small-molecule hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor. It was developed by GSK for the treatment of anemia in patients with chronic kidney disease (CKD). In patients with CKD, the diseased kidney cannot induce erythropoietin (EPO) production in response to hypoxia or anemia. As a potent inhibitor of PHD1, PHD2 and PHD3 (≥ 1000-fold selectivity), daprodustat leads to the stabilization of cellular HIF1α and HIF2α and the induction of erythropoiesis. A phase 3 clinical trial (NCT02879305) found that in patients with CKD undergoing dialysis, daprodustat was non-inferior to erythropoiesis-stimulating agents regarding the change in the hemoglobin level from baseline and cardiovascular outcomes.
1.HIF-PHI Activity: Daprodustat inhibits the activity of hypoxia-inducible factor prolyl hydroxylase enzymes (HIF-PHs). These enzymes normally break down HIF in the presence of oxygen, preventing HIF from activating erythropoietin production. By inhibiting HIF-PHs, Daprodustat allows HIF to accumulate and become active, leading to increased erythropoietin production.
2.Erythropoiesis Stimulation: With higher levels of erythropoietin, Daprodustat promotes the formation of new red blood cells (erythropoiesis) in the bone marrow. This can help improve hemoglobin levels and alleviate anemia, a condition characterized by a deficiency of red blood cells or hemoglobin.
Daprodustat was being investigated as a potential alternative to traditional erythropoietin-stimulating agents (ESAs) for the management of anemia in CKD patients. ESAs, such as erythropoietin, are commonly used to stimulate red blood cell production in CKD patients with anemia. However, HIF-PHIs like Daprodustat offered a different mechanism of action and could potentially reduce the frequency of ESA injections.
1kg/bag or 2kg/bag or 5kg/bag or 10kg/bag or according to customer’s requirements.
Daprodustat is a small-molecule hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor. It was developed by GSK for the treatment of anemia in patients with chronic kidney disease (CKD). In patients with CKD, the diseased kidney cannot induce erythropoietin (EPO) production in response to hypoxia or anemia. As a potent inhibitor of PHD1, PHD2 and PHD3 (≥ 1000-fold selectivity), daprodustat leads to the stabilization of cellular HIF1α and HIF2α and the induction of erythropoiesis. A phase 3 clinical trial (NCT02879305) found that in patients with CKD undergoing dialysis, daprodustat was non-inferior to erythropoiesis-stimulating agents regarding the change in the hemoglobin level from baseline and cardiovascular outcomes.
1.HIF-PHI Activity: Daprodustat inhibits the activity of hypoxia-inducible factor prolyl hydroxylase enzymes (HIF-PHs). These enzymes normally break down HIF in the presence of oxygen, preventing HIF from activating erythropoietin production. By inhibiting HIF-PHs, Daprodustat allows HIF to accumulate and become active, leading to increased erythropoietin production.
2.Erythropoiesis Stimulation: With higher levels of erythropoietin, Daprodustat promotes the formation of new red blood cells (erythropoiesis) in the bone marrow. This can help improve hemoglobin levels and alleviate anemia, a condition characterized by a deficiency of red blood cells or hemoglobin.
Daprodustat was being investigated as a potential alternative to traditional erythropoietin-stimulating agents (ESAs) for the management of anemia in CKD patients. ESAs, such as erythropoietin, are commonly used to stimulate red blood cell production in CKD patients with anemia. However, HIF-PHIs like Daprodustat offered a different mechanism of action and could potentially reduce the frequency of ESA injections.
1kg/bag or 2kg/bag or 5kg/bag or 10kg/bag or according to customer’s requirements.
