Erenzo is a first-in-class, orally administered hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. It stimulates erythropoiesis by increasing endogenous erythropoietin (EPO) production, improving iron utilization, and counteracting inflammation-mediated suppression of hemoglobin synthesis through downregulation of hepcidin.
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Erenzo is indicated for the treatment of symptomatic anemia in adult patients with chronic kidney disease (CKD).
Roxadustat, the active ingredient in Erenzo, is an orally bioavailable HIF-PH inhibitor (HIF-PHI) with anti-anemic properties. By inhibiting HIF-PH enzymes responsible for HIF degradation under normoxic conditions, roxadustat stabilizes HIF transcription factors and enhances their activity.
Activation of the HIF pathway results in:
Increased endogenous erythropoietin production
Enhanced erythropoiesis
Reduced hepcidin expression
Improved iron absorption, transport, and utilization
Increased hemoglobin (Hb) levels
Clinical studies have demonstrated that roxadustat induces coordinated erythropoiesis, increasing red blood cell counts while maintaining EPO levels within or near physiological ranges. This effect is observed in both dialysis-dependent and non-dialysis CKD patients, including those with inflammation, without the need for supplemental intravenous iron.
Additionally, roxadustat improves iron metabolism by increasing serum transferrin levels, enhancing intestinal iron absorption, and mobilizing stored iron. A significant reduction in cholesterol levels from baseline has also been observed, irrespective of concurrent statin or lipid-lowering therapy.
Dosing frequency: Oral administration three times per week, on non-consecutive days
Target hemoglobin: Maintain Hb levels between 10–12 g/dL
Standard starting dose: 50 mg, three times weekly
Body-weight–based dosing:
<100 kg: 70 mg three times weekly
≥100 kg: 100 mg three times weekly
Starting dose: 70 mg or 100 mg, three times weekly
Subsequent adjustments based on clinical response and Hb levels
Adjust dose according to recommended stepwise titration guidelines
Maintain each adjusted dose for at least 4 weeks
If Hb rises rapidly (>2.0 g/dL within 4 weeks), reduce dose or temporarily discontinue therapy
Available dose sequence:
20 mg → 40 mg → 50 mg → 70 mg → 100 mg → 150 mg → 200 mg → 250 mg → 300 mg → 400 mg
(400 mg only for dialysis-dependent CKD patients)
If ≥24 hours remain before the next scheduled dose, take the missed dose immediately
If <24 hours remain, skip the missed dose
Do not take two doses on the same day
Children: Not indicated
Severe hepatic impairment: Not recommended
(Except lanthanum carbonate)
Risk:
AUC decreased by 46–67%
Cmax decreased by 52–66%
Recommendation: Take Erenzo at least 1 hour after such products
Risk:
AUC increased by 2.3-fold
Cmax increased by 1.4-fold
Recommendation: Adjust Erenzo dose based on Hb monitoring
(e.g., simvastatin, rosuvastatin, atorvastatin)
Risk: Increased AUC and Cmax
Recommendation: Follow Hb-guided dose-adjustment protocols
Store below 30°C
Keep in a cool, dry place, protected from light and moisture
Keep out of reach of children
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