Deferasirox

What is Deferasirox?

• Deferasirox (Exjade) is an iron chelator used for the treatment of chronic iron overload.

What are the uses of this medicine?

Exjade is a prescription medicine that is used to treat:

• people 2 years of age and older who have an increased amount of iron in their blood for a long period of time (chronic), caused by repeated blood transfusions
• certain people 10 years of age or older with thalassemia who have an increased amount of iron in their blood but who are not receiving regular blood transfusions

Limitations of Use:

• It is not known if Exjade is safe and effective when used with other medicines to treat an increased amount of iron in the blood.

How does this medicine work?

• Deferasirox (dee fer’ a sir ox) is an orally available iron chelating agent that is selective for ferric iron and binds iron with a high affinity.
• Deferasirox binds two iron molecules and is eliminated in the feces after hepatic metabolism by glucuronidation.
• Deferasirox also binds zinc and copper, but to a far lower extent than iron.
• In clinical trials in patients with transfusion related iron overload, deferasirox lowered both circulating and tissue (cardiac, liver) iron.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have certain kidney problems
• have high-risk myelodysplastic syndrome (MDS)
• have advanced cancer
• have a low platelet count
• are allergic to deferasirox or any of the ingredients in Exjade.

What drug interactions can this medicine cause?

• Do not take Exjade with aluminum-containing antacid preparations.
• Exjade increases the exposure of the CYP2C8 substrate repaglinide. Consider repaglinide dose reduction and monitor blood glucose levels.
• Avoid the use of Exjade with CYP1A2 substrate theophylline.
• Deferasirox increases exposure of busulfan. Monitor plasma concentrations of busulfan when coadministered with deferasirox to allow dose adjustment of busulfan as needed.

Is this medicine FDA approved?

• Initial U.S. Approval: 2005

How should this medicine be used?

Recommended Dosage:

• Transfusional Iron Overload: Initial dose for patients with estimated glomerular filtration rate (eGFR) greater than 60 mL/min/1.73 m2 is 20 mg per kg body weight once daily, as oral suspension. Calculate dose to the nearest whole tablet.
• Non-Transfusion-Dependent Thalassemia Syndromes : Initial dose for patients with eGFR greater than 60 mL/min/1.73 m2 is 10 mg per kg body weight once daily, as oral suspension. Calculate dose to the nearest whole tablet.

Administration

• Take Exjade exactly as your healthcare provider tells you to.
• Do not change your dose of Exjade or stop taking it unless your healthcare provider tells you to.
• Take Exjade 1 time every day, preferably at the same time every day.
• Take Exjade on an empty stomach at least 30 minutes before eating food.
• Do not chew Exjade tablets or swallow them whole.
• Place the prescribed number of Exjade tablets in a cup with water, orange juice, or apple juice. Stir to disperse the tablets in the liquid.
• If your prescribed dose of Exjade is less than 1 gram, use 3.5 ounces of liquid to disperse the tablets.
• If your prescribed dose of Exjade is 1 gram or more, use 7 ounces of liquid to disperse the tablets.
• Completely disperse the tablets until it becomes a fine suspension. Then drink the suspension right away.
• Do not disperse Exjade tablets in carbonated drinks or milk.
• After drinking the suspension, add a small amount of water, orange juice, or apple juice to the cup to disperse any remaining medicine, and then drink it.
• Do not take Exjade with aluminum-containing antacid products. See “Before taking Exjade.”
• Tell your healthcare provider if you or your child gain or lose any weight. Your or your child’s dose of Exjade may need to be adjusted.
• If you take the diabetes medicine repaglinide during treatment with Exjade, you may need to test your blood sugar (glucose) levels more often. Follow your healthcare provider’s instructions about how often to test your blood sugar during this time.
• Your healthcare provider should do blood and urine tests before, and during treatment to check how you respond to Exjade, and to monitor you for side effects. Your healthcare provider may change your dose, or temporarily or permanently stop Exjade if you have certain side effects.
• In people who have thalassemia, your healthcare provider will check the amount of iron in your liver before and during treatment with Exjade.
• If you or your child take too much Exjade, call your healthcare provider right away or go to the nearest hospital emergency room. Symptoms that can happen if you take too much Exjade include: stomach-area (abdominal) pain, diarrhea, nausea, and vomiting.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets for oral suspension: 125 mg, 250 mg, 500 mg.

This medicine is available in fallowing brand namesː

• Exjade

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea and nausea.
• Other common side effects in people with too much iron in their blood due to repeated blood transfusions include: vomiting, stomach-area (abdomen) pain, and an abnormal kidney function blood test.

Exjade can cause serious side effects, including:

• Kidney problems
• Liver problems
• Bleeding, ulcers, and tears of the stomach or intestine
• Effects on your bone marrow
• Serious allergic reactions
• Skin rash and severe skin reactions
• Hearing and vision problems

What special precautions should I follow?

• Exjade can cause acute kidney injury including renal failure requiring dialysis that has resulted in fatal outcomes. Measure serum creatinine in duplicate before starting therapy. Monitor renal function during Exjade therapy and reduce dose or interrupt therapy for toxicity.
• Exjade can cause hepatic injury, fatal in some patients. Monitor hepatic function. Reduce dose or interrupt therapy for toxicity.
• GI hemorrhage, including deaths, has been reported in Exjade-treated patients, especially in elderly patients who had advanced hematologic malignancies and/or low platelet counts. Risk may be greater in patients who are taking Exjade in combination with drugs that have known ulcerogenic or hemorrhagic potential.
• Neutropenia, agranulocytosis, worsening anemia, and thrombocytopenia, including fatal events, have been reported in patients treated with Exjade. monitor blood counts during Exjade therapy. Interrupt therapy for toxicity.
• Exjade has been associated with serious and fatal adverse reactions in the postmarketing setting among adults, predominantly in elderly patients. Monitor elderly and pediatric patients closely for toxicity.
• Exjade may cause serious hypersensitivity reactions (such as anaphylaxis and angioedema), with the onset of the reaction usually occurring within the first month of treatment. Discontinue Exjade for severe reactions and institute medical intervention.
• Severe Skin Reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) may occur. Discontinue Exjade.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hepatitis
• acute renal failure
• abdominal pain
• diarrhea
• nausea
• vomiting
• Hepatic and renal disorders
• liver enzyme and creatinine increased
• Fanconi syndrome

Management of overdosage:

• There is no specific antidote for Exjade.
• In case of overdose, it may be treated with induction of vomiting or gastric lavage, and by symptomatic treatment.

Can this medicine be used in pregnancy?

• There are no studies with the use of Exjade in pregnant women to inform drug-associated risks.

Can this medicine be used in children?

• The safety and effectiveness of Exjade have been established in pediatric patients 2 years of age and older for the treatment of transfusional iron overload
• Safety and effectiveness have not been established in pediatric patients less than 2 years of age for the treatment of transfusional iron overload.
• The safety and effectiveness of Exjade have been established in patients 10 years of age and older for the treatment of chronic iron overload with non-transfusion-dependent thalassemia (NTDT) syndromes.
• Safety and effectiveness have not been established in patients less than 10 years of age with chronic iron overload in NTDT syndromes.

What are the active and inactive ingredients in this medicine?

• Active ingredient: deferasirox
• Inactive ingredients: Crospovidone, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone (K30), silicone dioxide, and sodium lauryl sulphate.

Who manufactures and distributes this medicine?

• Distributed by: Novartis Pharmaceuticals Corporation, East Hanover, New Jersey

What should I know about storage and disposal of this medication?

• Store Exjade at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep the bottle closed tightly and away from moisture.
• Keep Exjade and all medicines out of the reach of children.

Arsenic Chelators

• Dimercaprol

Copper Chelators (for Wilson Disease)

• Dimercaprol
• Penicillamine
• Trientine
• Zinc

Iron Chelators

• Deferasirox
• Deferiprone
• Deferoxamine

Lead Chelators

• Dimercaprol
• EDTA
• Succimer

Mercury Chelators

• Dimercaprol

• Dailymed label info on Deferasirox
• FDA Deferasirox

Deferasirox Resources
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