Medicine Overview of Daprosis 2mg Tablet
_NAME_ is a hypoxia-inducible factor, prolyl hydroxylase inhibitor (HIF-PHI). The activity of HIF-PH enzymes controls intracellular levels of HIF, a transcription factor that regulates the expression of genes involved in erythropoiesis. Activation of the HIF pathway is important in the adaptive response to hypoxia to increase red blood cell production. Through the reversible inhibition of HIF-PH, Daprodustat stimulates a coordinated erythropoietic response that includes the increase of plasma endogenous erythropoietin (EPO) levels, regulation of iron transporter proteins and reduction of hepcidin (an iron regulator protein that is increased during inflammation in CKD). This results in improved iron bioavailability, increased Hb production and increased red cell mass.
_NAME_ is a hypoxia-inducible factor, prolyl hydroxylase inhibitor (HIF-PHI). The activity of HIF-PH enzymes controls intracellular levels of HIF, a transcription factor that regulates the expression of genes involved in erythropoiesis. Activation of the HIF pathway is important in the adaptive response to hypoxia to increase red blood cell production. Through the reversible inhibition of HIF-PH, Daprodustat stimulates a coordinated erythropoietic response that includes the increase of plasma endogenous erythropoietin (EPO) levels, regulation of iron transporter proteins and reduction of hepcidin (an iron regulator protein that is increased during inflammation in CKD). This results in improved iron bioavailability, increased Hb production and increased red cell mass.
_NAME_ is not indicated for use:
As a substitute for red blood cell transfusions in patients who require immediate correction of anemia.
For treatment of anemia of chronic kidney disease in patients who are not on dialysis.
Adults Not Being Treated with an Erythropoiesis-Stimulating Agent (ESA):
Pre-Treatment Hemoglobin Level less than 9 g/dL: 4 mg orally once daily
Pre-Treatment Hemoglobin Level 9 to 10 g/dL: 2 mg orally once daily
Pre-Treatment Hemoglobin Level greater than 10 g/dL: 1 mg orally once daily
Dosing based on adults being switched from an ESA:
Dose of _NAME_: 4 mg orally once daily
Epoetin alfa intravenous less than or equal to 2,000 units/week
Darbepoetin alfa subcutaneous/intravenous 20 to 30 mcg/4 weeks
Methoxy PEG-epoetin beta subcutaneous/intravenous 30 to 40 mcg/month
Dose of _NAME_: 6 mg orally once daily
Epoetin alfa intravenous greater than 2,000 to less than 10,000 units/week
Darbepoetin alfa subcutaneous/intravenous greater than 30 to 150 mcg/4 weeks
Methoxy PEG-epoetin beta subcutaneous/intravenous greater than 40 to 180 mcg/month
Dose of _NAME_: 8 mg orally once daily
Epoetin alfa intravenous greater than 2,000 to less than 10,000 units/week
Darbepoetin alfa subcutaneous/intravenous greater than 150 to 300 mcg/4 weeks
Methoxy PEG-epoetin beta subcutaneous/intravenous greater than 180 to 360 mcg/month
Dose of _NAME_: 12 mg orally once daily
Epoetin alfa intravenous greater than or equal to 20,000 units/week
Darbepoetin alfa subcutaneous/intravenous greater than 300 mcg/4 weeks
Methoxy PEG-epoetin beta subcutaneous/intravenous greater than 360 mcg/month
Maximum dose: 24 mg orally once daily
Hemodialysis or peritoneal dialysis
_NAME_ exposure not significantly impacted
Systemic exposure of _NAME_ metabolites was higher in patients with Stage 3-5 CKD than in those with normal renal function.
Exposures of metabolites were higher on non-dialysis days than on dialysis days.
With uncontrolled hypertension.
-NAME_ is a reversible inhibitor of the hypoxia-inducible factors (HIFs) polyhomeotic-like proteins 1 to 3 (IC50 in the low-nanomoles range), a set of enzymes that degrade HIFs in normal oxygen conditions. HIF inhibition results in the stabilization and nuclear accumulation of the HIF 1α and 2α transcription factors, leading to increased transcription of the HIF-responsive genes, including that encoding erythropoietin. -NAME_increases endogenous erythropoietin in a dose-dependent manner in 6 to 8 hours after administration. With repeated doses, the peak increase in reticulocyte count occurs in 7 to 15 days, with subsequent increases in red blood cell production. New hemoglobin steady-state levels are reached in several weeks after initial administration (∼4 weeks in patients using erythropoiesis-stimulating agents [ESAs] and ∼16 to 20 weeks in patients not using ESAs).
High blood pressure
Damage to the lining of the stomach, the tube that connects the mouth and stomach (esophagus), and intestines (gastrointestinal erosion).
CYP2C8 Inducers: CYP2C8 inducers (e.g., rifampin) may decrease _NAME_ exposure, which may result in loss of efficacy.
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