Daprodustat is used to treat anemia caused by chronic kidney disease (CKD) in patients who have been on dialysis for at least 4 months. This medicine works by increasing erythropoietin (protein) to help the body make more red blood cells. It is also used to lessen or avoid the need for blood transfusion.
Available in 1 mg, 2 mg, 4 mg, 6 mg, and 8 mg tablet strengths for once-daily oral administration, with or without food. Aprodust 2 should be taken orally exactly as prescribed by the physician. Swallow the tablet whole without chewing, crushing, or breaking it.
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Aprodust is indicated for the treatment of anemia due to CKD in adult patients who have been on dialysis for at least four months.
It should not be used:
Daprodustat is a hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI). HIF-PH enzymes regulate intracellular levels of hypoxia-inducible factor (HIF), a transcription factor involved in erythropoiesis. Activation of the HIF pathway plays a key role in the body’s adaptive response to low oxygen levels by promoting red blood cell production.
By reversibly inhibiting HIF-PH enzymes, Daprodustat increases endogenous erythropoietin (EPO) production, improves regulation of iron transport proteins, and lowers hepcidin levels, which are often elevated in chronic kidney disease (CKD). These effects enhance iron availability, stimulate hemoglobin synthesis, and increase red blood cell mass.
Daprodustat works by inhibiting HIF prolyl hydroxylase enzymes, which normally break down HIF under standard oxygen conditions. Inhibition of these enzymes stabilizes HIF-1α and HIF-2α transcription factors, increasing the expression of genes involved in erythropoiesis, including erythropoietin production.
Following administration, endogenous erythropoietin levels rise in a dose-dependent manner within approximately 6–8 hours. Repeated dosing leads to increased reticulocyte production within 7–15 days, followed by enhanced red blood cell formation. Stable hemoglobin levels are generally achieved within several weeks.
Not recommended for children
Exposure to Daprodustat remains generally similar in patients with normal or impaired renal function. Hemodialysis and peritoneal dialysis do not significantly affect drug exposure.
However, metabolite exposure may be increased in patients with advanced CKD, especially on non-dialysis days.
Strong CYP2C8 inhibitors such as gemfibrozil significantly increase Daprodustat exposure and are contraindicated.
Agents like rifampin may decrease Daprodustat levels and reduce therapeutic effectiveness.
Use during pregnancy is not recommended. Animal studies have demonstrated adverse fetal effects.
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