Deferasirox

Mechanism of action

Deferasirox is an oral chelator selective for ferric iron. It is a tridentate ligand: two molecules wrap one iron ion. The complex is excreted mainly in the faeces. Steady removal of iron lowers ferritin and the iron stored in the liver.

1. Repeated transfusions load the body with iron
2. Two deferasirox molecules wrap one ferric ion
3. The iron complex leaves mainly in the faeces
4. Ferritin and liver iron fall over months

Indications

• Chronic iron overload from blood transfusions, for example in thalassaemia or sickle cell disease Thalassemias (α and β) →
• Chronic iron overload in non-transfusion-dependent thalassaemia Thalassemias (α and β) →

Adverse effects

Common

• Diarrhoea, nausea, vomiting and abdominal pain
• Rash
• Rises in serum creatinine and liver enzymes

Contraindications

• Reduced kidney function below the label's eGFR limit
• Poor performance status, high-risk myelodysplastic syndrome or advanced cancer
• Low platelet count
• Hypersensitivity to deferasirox

Key interactions

Aluminium-containing antacids

Not taken together

Rifampicin, phenytoin, phenobarbital, ritonavir and bile acid sequestrants

Lower deferasirox levels; avoided

Repaglinide (CYP2C8) and theophylline (CYP1A2)

Their levels rise; dose review and closer monitoring

NSAIDs, corticosteroids, oral bisphosphonates and anticoagulants

Higher risk of gastrointestinal ulcers and bleeding

Hormonal contraceptives (CYP3A4)

May become less effective; non-hormonal contraception is advised

What is monitored

• Serum ferritin monthly, to guide treatment and avoid over-chelation
• Serum creatinine, eGFR, urinalysis and electrolytes
• Liver enzymes and bilirubin: often in the first month, then at least monthly
• Blood counts
• Hearing and eye examinations before treatment and periodically

Administration and safety

• Given by mouth at the same time each day, on an empty stomach or with a light meal
• Treatment is paused or adjusted when kidney or liver tests worsen
• Not restarted after a serious allergic or skin reaction

Pregnancy and breastfeeding

Human data are lacking and animal studies showed harm to offspring; it is used only if the benefit justifies the risk.

Nursing care

• Check kidney and liver results before each new supply
• Ask about black stools, vomiting blood or abdominal pain
• Teach the patient to report rash, fever, sore throat or changes in hearing and vision
• Keep hydration up, especially during vomiting or diarrhoea

Pharmacokinetics

Absorption

Oral; taken on an empty stomach or with a light, low-fat meal

Elimination

The iron complex is excreted mainly in the faeces

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Connections

← Back to the class: Chelating agents

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - DEFERASIROX- deferasirox tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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