Deferasirox

Deferasirox is an orally active chelator that is highly selective for iron (as Fe3+ ion). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Deferasirox promotes excretion of iron, primarily in the faeces. Deferasirox has low affinity for zinc and copper, and does not cause constant low serum levels of these metals.

• Chronic iron overload due to repeated blood transfusions
• Transfusion-dependent thalassemia
• Sickle cell disease and myelodysplastic syndrome

Deferasirox is an orally active chelator that is highly selective for iron. It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Deferasirox promotes excretion of iron, primarily in the faeces.

Deferasirox binds to excess iron in the body, forming a stable complex that is excreted mainly in the stools, reducing the risk of organ damage.

Adult - Transfusional Hemosiderosis: 20 mg/kg once daily orally; may increase by 5-10 mg based on serum ferritin; maximum 40 mg/kg/day.
Adult - Nontransfusion-Dependent Thalassemia: 10 mg/kg once daily.

Take once daily on an empty stomach at least 30 minutes before food. Disperse tablets in a glass of water, apple or orange juice (100-200 mL). Do not chew or swallow tablets whole.

If you miss a dose of Deferasirox, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose. Do not double the dose.

Common: Nausea, headache, vomiting, rash, abdominal pain, constipation, itching, increased liver enzymes, abdominal distension, diarrhea.
Serious: Cytopenias, gastrointestinal ulceration and hemorrhage, Stevens-Johnson syndrome (SJS), auditory and ocular disturbances.

Gastrointestinal bleeding, ulceration and irritation may occur; caution with NSAIDs, corticosteroids, oral bisphosphonates and anticoagulants. Monitor blood counts. Discontinue if serious hypersensitivity reactions occur. Caution while driving (drowsiness, dizziness).

Hypersensitivity; Creatinine clearance <40 mL/min or serum creatinine >2x ULN.

Aluminium-containing antacids: Do not use (may chelate aluminium).
CYP3A4 substrates (cyclosporine, simvastatin, hormonal contraceptives, midazolam): Caution required.
Rifampicin, phenytoin, phenobarbital, ritonavir: Dose increase may be considered.

It is not known whether it is safe to consume alcohol with Deferasirox. Please consult your doctor.

Pregnancy Category C. Deferasirox may be unsafe during pregnancy. Animal studies have shown harmful effects on the developing baby. Use only if clearly needed.

It is not known whether Deferasirox is excreted in human milk. Caution should be exercised when administered to a nursing woman.

Safety and efficacy in pediatric patients aged 2 years and over is similar to that of adult patients.

Elderly patients are at increased risk for Deferasirox toxicity due to greater frequency of decreased hepatic, renal, or cardiac function.

Renal impairment: CrCl 40-60 mL/min: Reduce starting dose by 50%; CrCl <40 mL/min or serum Cr >2x ULN: Do not use.
Hepatic impairment: Mild (Child-Pugh A): No dose adjustment; Moderate (Child-Pugh B): 50% dose reduction; Severe (Child-Pugh C): Avoid use.

The maximal dose of Deferasirox is 40 mg/kg body weight. There is no information about overdose.

Store in a dry place below 25°C, protect from light. Keep out of reach of children.

Deferasirox