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daprodustat
- Development stage
- Approved
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Daprodustat is a small-molecule hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor developed for the treatment of anemia due to chronic kidney disease (CKD), specifically in adults who have been on dialysis for at least four months. By reversibly inhibiting the oxygen-sensing prolyl hydroxylase enzymes (PHD1, PHD2, and PHD3), daprodustat stabilizes hypoxia-inducible factors HIF-1α and HIF-2α. This leads to increased transcription of erythropoietin (EPO) and other genes involved in erythropoiesis and iron metabolism, resulting in elevated red blood cell production and improved hemoglobin levels. Daprodustat is taken orally and has demonstrated non-inferiority to recombinant human erythropoietin regarding efficacy and cardiovascular outcomes in clinical trials[1][3][4][5][8].
- Brand names
- JesduvroqDuvroq
- Other names
- daprodustatGSK1278863GSK-1278863GSK 1278863UNII-JVR38ZM64BUNII-JVR-38ZM64BUNII-JVR 38ZM64B
02
Targets
PHD1 (Prolyl hydroxylase domain-containing protein 1)EGLN1 (Prolyl hydroxylase domain-containing protein 2)PHD3 (Prolyl hydroxylase domain-containing protein 3)
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