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Drugs reference index «Deferasirox»


Pronunciation: (de-FER-a-sir-ox)Class: Chelating agent

Trade Names:Exjade- Tablets for oral suspension 125 mg- Tablets for oral suspension 250 mg- Tablets for oral suspension 500 mg


Active chelating agent that has a high affinity for binding with iron.



Bioavailability is 70%. Median time to T max is approximately 1.5 to 4 h. C max and AUC increase approximately linearly.


Protein binding is approximately 99% and almost exclusively to serum albumin. Vd is approximately 14 L.


Major metabolic pathway is glucuronidation, with subsequent biliary excretion. Deferasirox is deconjugated in the intestine and undergoes enterohepatic recirculation.


Primarily excreted in feces (84%) with minimal renal excretion (8%). Elimination t ½ ranges from 8 to 16 h.

Special Populations


In children younger than 6 yr of age, systemic exposure was approximately 50% lower than in adults.


Cl appears to be moderately lower (17.5%) in women than in men.

Renal/Hepatic Function Impairment

Has not been studied in patients with renal or hepatic function impairment.

Indications and Usage

Treatment of chronic iron overload caused by blood transfusions (transfusional hemosiderosis) in patients 2 yr of age and older.


Standard considerations.

Dosage and Administration

Adults and children 2 yr of age and older Initial dose

PO Start when patient has evidence of chronic iron overload and a serum ferritin consistently greater than 1,000 mcg/L. Initial dose is 20 mg/kg.

Maintenance dose

PO Adjust the dose as needed every 3 to 6 mo based on serum ferritin trends. Make dose adjustments in steps of 5 or 10 mg/kg based on patient's response and therapeutic goals. Consider interrupting therapy if serum ferritin consistently falls below 500 mcg/L. Dosage should not exceed 30 mg/kg/day.

Dosage adjustment for renal function impairment

Dose reduction, interruption, or discontinuation should be considered for increases in serum creatinine. If there is a progressive increase in serum creatinine beyond the age-appropriate ULN, interrupt deferasirox therapy. Once creatinine has returned to within the normal range, therapy may be restarted at a lower dose followed by gradual dose escalation. For adult patients, reduce the daily dose by 10 mg/kg if serum creatinine increases to more than 33% above the average of the pretreatment measurements at 2 consecutive visits, and if the increase cannot be attributed to other causes. For children, reduce the dose by 10 mg/kg if serum creatinine levels rise above the age-appropriated ULN at 2 consecutive visits.

General Advice

  • Administer once daily on an empty stomach at least 30 min before food, preferably at the same time each day.
  • Tablets are for suspension only. Do not chew or swallow whole.
  • Calculate dose to the nearest whole tablet.
  • Completely disperse tablet by stirring in water, orange juice, or apple juice until a fine suspension is obtained. Disperse doses less than 1 g in 3.5 oz of liquid, and disperse doses of 1 g or more in 7 oz of liquid. Drink suspension immediately.
  • Resuspend any residue in a small volume of liquid and swallow.


Store between 59° to 86°F. Protect from moisture.

Drug Interactions

Aluminum-containing antacids

Avoid coadministration.

Other iron chelator therapy

Do not coadminister because safety has not been established.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Pyrexia (19%); headache (16%); fatigue (6%).


Rash (8%); urticaria (4%); leukocytoclastic vasculitis (postmarketing).


Nasopharyngitis (13%); pharyngolaryngeal pain (11%); pharyngitis (8%); acute tonsillitis, rhinitis (6%); ear infection (5%).


Abdominal pain (14%); diarrhea (12%); nausea (11%); vomiting (10%); upper abdominal pain (8%).


Acute renal failure (postmarketing).


Cytopenias including agranulocytosis, neutropenia, and thrombocytopenia (postmarketing).


Hepatic failure, some with fatal outcome (postmarketing).


Anaphylaxis and angioedema (postmarketing).

Lab Tests

Increased creatinine (38%); increased ALT (8%).


Arthralgia (7%); back pain (6%).


Increased creatinine (11%).


Cough (14%); respiratory tract infection (10%); bronchitis (9%).


Influenza (11%).



Closely monitor proteinuria. Monitor serum ferritin monthly. Monitor serum creatinine before initiating therapy and monthly thereafter. Monitor liver and renal function monthly during treatment. Auditory and ophthalmic testing are recommended before the start of treatment and every 12 mo thereafter.


Category B .




Safety and efficacy not established in children younger than 2 yr of age.


Use with caution, usually starting at the low end of the dosage range because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.


Serious hypersensitivity reactions (eg, anaphylaxis, angioedema) have been reported, with the onset of the reaction occurring in the majority of cases within the first month of treatment.

Renal Function

Dose-dependent increases in serum creatinine have been reported.

Hepatic Function

There have been postmarketing reports of hepatic failure, some with fatal outcome.

Special senses

Auditory disturbances (eg, decreased hearing, high-frequency hearing loss) and ocular disturbances (eg, cataract, elevations in IOP, lens opacities, retinal disorders) have been reported.



Diarrhea, hepatitis, nausea.

Patient Information

  • Advise patient to take deferasirox once daily on an empty stomach at least 30 min prior to food, preferably at the same time each day.
  • Advise patient not to chew or swallow the tablet whole.
  • Instruct patient to completely disperse the tablet in water, orange juice, or apple juice, and to drink the resulting suspension immediately.
  • Instruct patient to resuspend any residue in a small volume of liquid and swallow.
  • Caution patient to not take deferasirox with aluminum-containing antacids.
  • Caution patients that if they experience dizziness to exercise caution when driving or operating machinery.

Copyright © 2009 Wolters Kluwer Health.

  • Deferasirox MedFacts Consumer Leaflet (Wolters Kluwer)
  • deferasirox Advanced Consumer (Micromedex) - Includes Dosage Information
  • Exjade Prescribing Information (FDA)
  • Exjade Consumer Overview

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