Adult Dosing
Chronic transfusional iron overload
- Start 20 mg/kg PO qd, administer the dose 30 mins before meals preferably at the same time each day
- Adjust dosage by 5-10 mg/kg q3-6 months based on serum ferritin levels if necessary
- Max: 40 mg/kg/day
Chronic iron overload with non-transfusion dependent thalassemia syndrome
- Start 10 mg/kg PO qd, administer the dose 30 mins before meals preferably at the same time each day
- Adjust dosage as per serum ferritin levels and LIC
- Following 6 months, if LIC >7 mg Fe/g dw, increase dose to 20 mg/kg/day; if LIC = 3-7 mg Fe/g dw, continue therapy (Max 10 mg/kg/day); if LIC <3 mg Fe/g dw interrupt therapy; if LIC >5 mg Fe/g dw, restart therapy
- Max: 20 mg/kg/day
Notes:- Do not chew or swallow the tablet, disperse completely by stirring in water/orange juice/apple juice until fine suspension is obtained
- Disperse doses <1 g in 3.5 ounces of liquid and doses
1 g in 7 ounces of liquid - Check baseline serum ferritin and iron levels prior to therapy
Pediatric Dosing
- Safety and effectiveness in pediatric patients <2 yrs of age have not been established
Chronic transfusional iron overload
Children >2 yrs
- Start 20 mg/kg PO qd, administer the dose 30 mins before meals preferably at the same time each day
- Adjust dosage by 5-10 mg/kg q3-6 months based on serum ferritin levels if necessary
- Max: 40 mg/kg/day
Chronic iron overload with non-transfusion dependent thalassemia syndrome
Children >10 yrs
- Start 10 mg/kg PO qd, administer the dose 30 mins before meals preferably at the same time each day
- Adjust dosage as per serum ferritin levels and LIC
- Following 6 months, if LIC >7 mg Fe/g dw, increase dose to 20 mg/kg/day; if LIC = 3-7 mg Fe/g dw, continue therapy (Max 10 mg/kg/day); if LIC <3 mg Fe/g dw interrupt therapy; if LIC >5 mg Fe/g dw, restart therapy
- Max: 20 mg/kg/day
Notes:- Do not chew or swallow the tablet, disperse completely by stirring in water/orange juice/apple juice until fine suspension is obtained
- Disperse doses <1 g in 3.5 ounces of liquid and doses 1 g in 7 ounces of liquid
- Check baseline serum ferritin and iron levels prior to therapy
[Outline]
See Supplemental Patient Information
- Cases of acute renal failure (post-marketing) have been reported. Monitor serum creatinine and/or creatinine clearance in patients with increased risk of complications, advanced age, having co-morbid conditions, or receiving drugs that decrease renal function. Closely monitor the renal functions in patients with CrCl between 40 and <60 mL/min especially in patients with increased risk factors for renal impairment such as severe infections, dehydration, or concomitant drugs
- Closely monitor serum creatinine and/or creatinine clearance prior to initiation of therapy and monthly thereafter; monitor creatinine and/or creatinine clearance weekly for the first month and then monthly thereafter in patients with underlying renal impairment or risk factors for renal impairment [US Black Box Warning]
- Cases of hepatic failure (post-marketing) have been reported, mostly in patients with significant comorbidities, including liver cirrhosis and multiorgan failure. Most of these events occurred in patients >55 yrs of age. Monitor serum transaminases and bilirubin prior to initiation of therapy, every two weeks during the first month and monthly thereafter
- Fatal GI hemorrhages, especially in elderly patients who had advanced hematologic malignancies and/or low platelet counts, have been reported
- During therapy, physicians and patients should remain alert for signs and symptoms of GI ulceration and hemorrhage and promptly initiate additional evaluation and treatment if a serious GI adverse event is suspected
- Agranulocytosis, neutropenia, and thrombocytopenia, including cases with fatal outcomes, have been reported (post-marketing). Monitor blood counts regularly. Interrupt treatment if the patient develops unexplained cytopenia, elucidate the cause of cytopenia and re-initiate the therapy
- Serious hypersensitivity reactions (such as anaphylaxis and angioedema) may occur within the first month of treatment; if severe reactions occur, discontinue deferasirox and institute appropriate medical intervention
- Stevens-Johnson syndrome (SJS) and erythema multiforme have been reported with therapy. Discontinue the therapy If SJS or erythema multiforme is suspected
- For rashes of mild to moderate severity, deferasirox may be continued without dose adjustment because the rash often resolves spontaneously. If severe, interrupt therapy and consider reintroduction at a lower dose in combination with a short course of oral steroids
- Deferasirox may cause decreased serum ferritin and liver iron concentration. Serious adverse reactions, including fatal outcomes, have been reported when administered to elderly patients, and in patients with complications from underlying conditions or very advanced disease
- Measure serum ferritin monthly to assess response to therapy and to evaluate for the possibility of over chelation of iron. Perform laboratory monitoring of renal and hepatic functions
- Auditory disturbances (eg, decreased hearing, high-frequency hearing loss) and ocular disturbances (eg, cataracts, elevations in IOP, lens opacities, retinal disorders) have been reported
Cautions: Use cautiously in
- Hepatic impairment
- Renal impairment
- Hematological disorders
- History of GI hemorrhage
- Malignancy
- Co-administration with medications metabolized by CYP3A4 and CYP2C8
- Concomitant use of potent UGT inducers (increase initial dose and monitor serum ferritin levels)
- Concurrent use of NSAIDs, corticosteroids, oral bisphosphonates, or anticoagulants
- Elderly patients >55 yrs with MDS
- Elderly patients with low platelet counts
Supplemental Patient Information
- Do not chew or swallow the tablets whole
- Advise patients who develop diarrhea or vomiting to maintain adequate hydration
- Caution patients against taking deferasirox and aluminum-containing antacids simultaneously
- Caution against driving or operating machinery if patients experience dizziness
- Instruct patients to have blood tests, auditory and ophthalmic testing before initiation of therapy and thereafter at regular intervals
Pregnancy Category:C
Breastfeeding: Safety unknown. Manufacturer advises caution when administered in nursing mothers due to the potential for serious adverse reactions in breastfed infants.
