Chronic iron overload due to blood transfusions: in patients ≥2 years of age
Chronic iron overload in non-transfusion-dependent thalassemia syndromes: in patients ≥10 years of age

Chelating Agent
Deferasirox is an orally active chelator that is highly selective for iron (Fe (3+)). Deferasirox promotes excretion of iron, primarily in the feces.

Distribution
Protein binding: approximately 99% to albumin
Metabolism
Hepatic via glucuronidation by UGT1A1 (primarily) and UGT1A3; minor oxidation by CYP450; undergoes enterohepatic recirculation
Excretion
1. Deferasirox and its metabolites are primarily excreted in the feces (84%) and renal excretion is minimal (8%).
2. Elimination half-life: 8 to 16 hours

1. Known hypersensitivity to deferasirox or any component of the formulation
2. eGFR <40 mL/minute/1.73 m2
3. High-risk myelodysplastic syndromes (MDS); patients with other hematological and nonhematological malignancies who are not expected to benefit from chelation therapy (due to rapid progression of their disease)

Information related to the use of deferasirox in pregnant women is limited. Use is not recommended.

Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends a decision be made to discontinue breastfeeding or to discontinue the drug, taking into account the importance of treatment to the mother.

Chronic iron overload due to blood transfusions:
1. Initial: 14 mg/kg once daily
2. Maintenance:
(1) Adjust dose every 3 to 6 months based on serum ferritin trends; adjust by 3.5 or 7 mg/kg/day
(2) Doses up to 28 mg/kg/day may be considered for serum ferritin levels persistently >2,500 mcg/L and not decreasing over time (doses >28 mg/kg/day are not recommended).
(3) If serum ferritin falls to <1,000 mcg/L at 2 consecutive visits, consider dose reduction (especially if dose is >17.5 mg/kg/day). If serum ferritin falls to <500 mcg/L, interrupt therapy and continue monitoring monthly.

Chronic iron overload in non-transfusion-dependent thalassemia syndromes:
1. Initial: 7 mg/kg once daily. Consider increasing to 14 mg/kg once daily after 4 weeks if baseline hepatic iron concentration is >15 mg Fe/g dry weight.
2. Maintenance:
(1) If serum ferritin is <300 mcg/L: Interrupt therapy and obtain hepatic iron concentration
(2) If hepatic iron concentration <3 mg Fe/g dry weight: Interrupt therapy; resume treatment when hepatic iron concentration is >5 mg Fe/g dry weight
(3) If hepatic iron concentration 3 to 7 mg Fe/g dry weight: Continue treatment at a dose of no more than 7 mg/kg/day
(4) If hepatic iron concentration >7 mg Fe/g dry weight: Increase dose up to 14 mg/kg/day; Maximum dose: 14 mg/kg/day

Use the minimum effective dose to achieve a trend of decreasing ferritin and to maintain iron burden in the target range.

1. eGFR >60 mL/minute/1.73 m2: No dosage adjustment necessary.
2. eGFR 40 to 60 mL/minute/1.73 m2: Initial: Reduce dose by 50%.
3. eGFR <40 mL/minute/1.73 m2: Use is contraindicated.

1. Mild impairment (Child-Pugh class A): No dosage adjustment necessary; monitor closely
2. Moderate impairment (Child-Pugh class B): Reduce dose by 50%; monitor closely
3. Severe impairment (Child-Pugh class C): Avoid use