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deferasirox

V03AC03

Forms & Strengths

Tablets for oral suspension: 125 mg, 250 mg, 500 mg
Film-coated tablets: 90 mg, 180 mg, 360 mg

Adult Dosing

Initial dose: 14 mg/kg once daily for transfusional iron overload
Non-transfusion-dependent thalassemia: 7 mg/kg once daily
Adjust based on serum ferritin trends and monthly monitoring

Pediatric Dosing

Approved for pediatric patients aged 2 years and older
Initial dose same as adults: 14 mg/kg once daily for transfusional iron overload
Dose adjustments based on efficacy and monthly safety parameters

Indications

Chronic iron overload due to frequent blood transfusions (transfusional hemosiderosis)
Chronic iron overload in non-transfusion-dependent thalassemia syndromes aged 10 years and older

Mechanism of Action

Terdentate iron chelator that binds with high affinity to trivalent iron (Fe3+)
Forms complexes primarily excreted via the feces, reducing iron accumulation in organs

Contraindications

Estimated creatinine clearance < 40 mL/min or serum creatinine > 2 times the age-related upper limit of normal
High-risk myelodysplastic syndromes, advanced malignancies, or platelet counts < 50 x 10^9/L
Known hypersensitivity to deferasirox or its excipients

Adverse Reactions

Gastrointestinal disturbances (abdominal pain, nausea, vomiting, diarrhea)
Elevated serum creatinine and acute renal failure
Elevated liver transaminases and hepatic failure
Skin rash and hypersensitivity reactions
Auditory and ocular disturbances

Drug Interactions

Antacids containing aluminum should not be co-administered
Substrates of CYP3A4 (e.g., cyclosporine, simvastatin, hormonal contraceptives) may have decreased exposure
Concomitant use with strong CYP inducers (e.g., rifampin, phenytoin) may decrease deferasirox efficacy
Increased risk of gastrointestinal ulceration or hemorrhage with NSAIDs, corticosteroids, or oral bisphosphonates

Curated Content: Needs Vetting Before Put to Clinical Use