Therapeutic Classification: antidotes
Pharmacologic Classification: chelating agents
Absorption: Well absorbed (70%) following oral administration; absorption is less in children.
Distribution: Unknown.
Protein Binding: 99%.
Metabolism/Excretion: Mostly metabolized by the liver, followed by enterohepatic recycling. 84% excreted in feces (deferasirox and metabolites); minimal renal excretion.
Half-Life: 8–16 hr.
Chronic Iron Overload Due to Blood Transfusions
- PO (Adults and Children ≥2 yr): Exjade: 20 mg/kg once daily; adjusted by 5–10 mg/kg every 3–6 mo on the basis of serum ferritin levels (not to exceed 40 mg/kg/day); Jadenu: 14 mg/kg once daily; adjusted by 3.5–7 mg/kg every 3–6 mo on the basis of serum ferritin levels (not to exceed 28 mg/kg/day).
Hepatic Impairment
- (Adults and Children ≥2 yr): Moderate hepatic impairment: ↓initial dose by 50%.
Renal Impairment
- (Adults and Children ≥2 yr): CCr 40–60 mL/min: ↓initial dose by 50%.
Chronic Iron Overload in Non-Transfusion-Dependent Thalassemia Syndromes
- PO (Adults and Children ≥10 yr): Exjade: 10 mg/kg once daily; if baseline liver iron concentration (LIC) >15 mg/g of liver dry weight, consider ↑ dose to 20 mg/kg/day after 4 wk. If liver iron concentration remains >7 mg/g of liver dry weight after 6 mo, ↑ dose to 20 mg/kg/day (maximum dose). If LIC is 3–7 mg/g of liver dry weight after 6 mo, continue therapy with no more than 10 mg/kg/day. When LIC <3 mg/g of liver dry weight, may discontinue therapy (restart when liver iron concentration >5 mg/g of liver dry weight); Jadenu: 7 mg/kg once daily; if baseline LIC >15 mg/g of liver dry weight, consider ↑ dose to 14 mg/kg/day after 4 wk. If LIC remains >7 mg/g of liver dry weight after 6 mo, ↑ dose to 14 mg/kg/day (maximum dose). If LIC is 3–7 mg/g of liver dry weight after 6 mo, continue therapy with no more than 7 mg/kg/day. When LIC <3 mg/g of liver dry weight, may discontinue therapy (restart when LIC >5 mg/g of liver dry weight).
Hepatic Impairment
- (Adults and Children ≥10 yr): Moderate hepatic impairment: ↓initial dose by 50%.
Renal Impairment
- (Adults and Children ≥2 yr): CCr 40–60 mL/min: ↓initial dose by 50%.
