Vadadustat

Research use only, not for human use.

Vadadustat (PG-1016548, AKB-6548) is a novel, potent, orally active HIF-PH inhibitor in development for the treatment of anemia in both nondialysis-dependent (NDD) and dialysis-dependent CKD.

Vadadustat (PG-1016548, AKB-6548) is a novel, potent, orally active HIF-PH inhibitor in development for the treatment of anemia in both nondialysis-dependent (NDD) and dialysis-dependent CKD; induces endogenous erythropoietin synthesis and enhances iron mobilization. Anemia Phase 3 Clinical.(In Vitro):Vadadustat induces endogenous erythropoietin synthesis and enhances iron mobilization. Vadadustat is well-tolerated in healthy volunteers and patients with chronic kidney disease, where it increases reticulocytes, plasma EPO, and Hb levels in a dose-dependent manner. The increase in plasma EPO levels seen with vadadustat is comparable in magnitude to that occurring physiologically at moderate altitude and shows a normal diurnal pattern with a return to baseline levels prior to the next dose. Vadadustat improves iron homeostasis by decreasing hepcidin and increasing transferrin levels. once-daily oral administration of vadadustat, titrated to increase and maintain Hb in the target range, may provide multiple advantages over conventional ESAs. Vadadustat is observed to have a half-life of approximately 4.5 hours. Overall, patients demonstrate an increase in Hb levels, from 9.91 g/dL at baseline to 10.54 g/dL by day 29. Ferritin levels decrease from 334.1 ng/mL at baseline to 271.7 ng/mL by day 29.

Vadadustat induces endogenous erythropoietin synthesis and enhances iron mobilization. Vadadustat is well-tolerated in healthy volunteers and patients with chronic kidney disease, where it increases reticulocytes, plasma EPO, and Hb levels in a dose-dependent manner. The increase in plasma EPO levels seen with vadadustat is comparable in magnitude to that occurring physiologically at moderate altitude and shows a normal diurnal pattern with a return to baseline levels prior to the next dose. Vadadustat improves iron homeostasis by decreasing hepcidin and increasing transferrin levels. once-daily oral administration of vadadustat, titrated to increase and maintain Hb in the target range, may provide multiple advantages over conventional ESAs. Vadadustat is observed to have a half-life of approximately 4.5 hours. Overall, patients demonstrate an increase in Hb levels, from 9.91 g/dL at baseline to 10.54 g/dL by day 29. Ferritin levels decrease from 334.1 ng/mL at baseline to 271.7 ng/mL by day 29.

——

PG-1016548 | PG1016548 | PG 1016548 | AKB-6548

Angiogenesis

HIF/HIF Prolyl-hydroxylase

HIF-PH

Other Indications

Anemia

1000025-07-9

306.70114

C14H11ClN2O4

>98% (HPLC)

DMSO: ≥ 33 mg/mL

O=C(O)CNC(C1=NC=C(C2=CC=CC(Cl)=C2)C=C1O)=O

Glycine, N-[[5-(3-chlorophenyl)-3-hydroxy-2-pyridinyl]carbonyl]-

(-20℃)

With Ice Pack

≥ 2 years