AieruiZhu®Roxadustat Capsules

1. Indications and Usage
Anemia in Chronic Kidney Disease (CKD): Treatment of anemia due to CKD, including patients both on dialysis (Dialysis-Dependent, DD) and not on dialysis (Non-Dialysis-Dependent, NDD) .
2. Dosage and Administration
Administration: Oral administration. Can be taken with or without food. For patients on hemodialysis or peritoneal dialysis, it can be administered at any time relative to the dialysis session .
Starting Dose:
Dialysis Patients: 100 mg (for weight 45–60 kg) or 120 mg (for weight ≥60 kg) three times a week (TIW) .
Non-Dialysis Patients: 70 mg (for weight 40–<60 kg) or 100 mg (for weight ≥60 kg) three times a week (TIW) .
Dose Adjustment: Hemoglobin (Hb) should be monitored every 2 weeks initially, then every 4 weeks once stable. Dosage is adjusted to maintain Hb levels between 100–120 g/L .
3. Mechanism of Action
Roxadustat is an oral inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH). By inhibiting PHD enzymes (PHD1, PHD2, PHD3), it stabilizes HIF-α.
This leads to increased endogenous production of erythropoietin (EPO) and improves iron metabolism (mobilization and utilization), thereby stimulating red blood cell production .
4. Safety and Warnings
Contraindications: Hypersensitivity to the active substance or excipients; Pregnancy; Breastfeeding .
Hypertension: Blood pressure should be monitored regularly, especially in patients with poorly controlled hypertension .
Thrombosis Risk: Rapid increase in Hb levels may increase the risk of thrombotic events; regular monitoring is required .
Liver Impairment: Caution is advised in moderate hepatic impairment; not recommended in severe hepatic impairment .
5. Adverse Reactions
Common adverse reactions (incidence >5%) include hypertension, hyperkalemia, nausea, diarrhea, headache, fatigue, and increased liver enzymes (ALT/AST) .
6. Drug Interactions
Prohibited: Should not be used concomitantly with Erythropoiesis-Stimulating Agents (ESAs) .
Phosphate Binders/Iron: Separate administration from phosphate binders (e.g., sevelamer, calcium acetate), oral iron, or antacids by at least 1 hour to avoid reduced absorption .
Statins: Roxadustat may increase the plasma exposure of statins (e.g., atorvastatin, rosuvastatin); dose reduction and monitoring for myopathy are recommended .
Metabolic Inhibitors: Co-administration with inhibitors of CYP2C8, UGT, or OAT transporters (e.g., gemfibrozil, probenecid) may increase Roxadustat exposure, requiring caution .
7. Pharmaceutical Information
Chemical Name: [[(4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl]amino]acetic acid .
Molecular Formula: C19H16N2O5 .
Molecular Weight: 352.34 .