Vadadustat

SKU: orb1227190

Description

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.

Key Properties

• CAS Number: 1000025-07-9
• MW: 306.70114
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₁ClN₂O₄
• SMILES: O=C(O)CNC(C1=NC=C(C2=CC=CC(Cl)=C2)C=C1O)=O
• Target: HIF/HIF Prolyl-hydroxylase
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Quick Database Links

Gene Symbol

HIF/HIF Prolyl-hydroxylase