Generic Name and Formulations:
Deferasirox 125mg, 250mg, 500mg; tabs for oral susp.
Novartis Pharmaceuticals Corp
Indications for EXJADE:
Chronic iron overload due to blood transfusions in patients ≥2yrs of age. Chronic iron overload in patients ≥10yrs of age with non-transfusion dependent thalassemia (NTDT) syndromes and with a liver iron concentration (LIC) of at least 5mg Fe per gram of dry weight and a serum ferritin >300mcg/L.
Adults and Children:
Calculate dose to nearest whole tab. Take on empty stomach at least 30mins before food. Do not chew or swallow tabs; disperse completely in water, orange juice or apple juice; drink immediately; resuspend remainder and drink. Transfusional iron overload: <2yrs: not established. ≥2yrs (with eGFR >60mL/min/1.73m2): initially 20mg/kg once daily; may adjust dose by 5 or 10mg/kg every 3–6 months based on serum ferritin levels or response. If inadequate control at 30mg/kg, may consider increasing up to max 40mg/kg. If serum ferritin <1000mcg/L at 2 consecutive visits, consider dose reduction (esp. if dose is >25mg/kg/day); interrupt therapy and continue monitoring if serum ferritin <500mcg/L. NTDT syndromes: <10yrs: not established. ≥10yrs (with eGFR >60mL/min/1.73m2): initially 10mg/kg once daily; if baseline LIC>15mg Fe/g dw, consider increasing dose to 20mg/kg/day after 4 weeks. Suspend therapy if serum ferritin <300mcg/L and obtain LIC to determine whether it has fallen to <3mg Fe/g dw. After 6 months, if LIC remains >7mg Fe/g dw, increase dose to max 20mg/kg/day. If after 6 months, LIC is 3–7mg Fe/g dw, continue with max 10mg/kg/day. When LIC is <3mg Fe/g dw, interrupt treatment and continue to monitor LIC. Restart when LIC rises again to >5mg Fe/g dw. Baseline hepatic impairment (moderate): reduce initial dose by 50%; (severe): avoid. Baseline renal impairment (eGFR 40–60mL/min/1.73m2): reduce initial dose by 50%; in pediatrics: caution and use the minimum effective dose; monitor frequently. Dose modifications for decreases in renal function, others: see full labeling.
eGFR <40mL/min/1.73m2. Poor performance status. High risk myelodysplastic syndromes. Advanced malignancies. Platelets <50x109/L.
Renal and hepatic failure. GI hemorrhage.
Risk of renal or hepatic injury/failure, GI hemorrhage; may be fatal (monitor). Advanced disease or co-morbid conditions. Increased risk of acute kidney injury or liver failure in pediatrics from acute illnesses associated with volume depletion or overchelation; monitor frequently. Renal tubular toxicity including Fanconi Syndrome. Obtain baseline serum ferritin level, monitor monthly and adjust dose accordingly. Measure serum creatinine in duplicate before starting therapy; monitor for eGFR changes, renal toxicity weekly during 1st month then at least monthly thereafter; more frequently if pre-existing renal disease or decreased function. Obtain urinalyses, serum electrolytes to evaluate renal tubular function. Measure serum transaminases, bilirubin before initiating therapy then every 2 weeks during 1st month, then monthly. Monitor blood counts; interrupt therapy if cytopenias develop. For NTDT syndromes: obtain LIC by liver biopsy prior to starting therapy, monitor LIC every 6 months. Monitor for severe skin reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis, DRESS, erythema multiforme); discontinue if suspected and do not restart. Do baseline auditory and ocular exams, then every 12 months; if disturbances occur, adjust dose or suspend therapy. Elderly: monitor. Pregnancy. Nursing mothers: not recommended.
Iron chelating agent.
Avoid aluminum-containing antacids, bile acid sequestrants (eg, cholestyramine, colesevelam, colestipol), or potent UGT inducers (eg, rifampicin, phenytoin, phenobarbital, ritonavir); if co-administration necessary consider increasing initial Exjade dose by 50% and monitor serum ferritin levels and clinical responses. Caution with drugs that have ulcerogenic or hemorrhagic potential (eg, NSAIDs, corticosteroids, oral bisphosphonates, anticoagulants) or drugs metabolized by CYP3A4 (eg, cyclosporine, simvastatin, hormonal contraceptives). Potentiates repaglinide (consider reducing repaglinide dose); monitor blood glucose levels. Caution with other CYP2C8 substrates (eg, paclitaxel). Avoid concomitant theophylline or other CYP1A2 substrates with narrow therapeutic index (eg, tizanidine). Concomitant other iron chelation therapy: not recommended.
Diarrhea, vomiting, nausea, abdominal pain, elevated serum creatinine, rash or skin reactions (may be severe); renal or hepatic injury/failure, GI hemorrhage, cytopenias (eg, agranulocytosis, neutropenia, thrombocytopenia, anemia), hypersensitivity reactions.
Hepatic (UGT1A1); ~99% protein bound.
Fecal, renal (minor).
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