Deferasirox is a once-daily, oral iron chelator used for the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years and older, and for the treatment of non-transfusion-dependent thalassemia (NTDT) syndromes with a liver iron concentration (LIC) of at least 5 mg Fe/g dry weight and a serum ferritin > 300 mcg/L. It is a tridentate ligand that binds iron with high selectivity in a 2:1 ratio.
Adult: Initial: 20 mg/kg body weight once daily. Maintenance: Adjust dose (range 10-40 mg/kg/day) every 3-6 months based on serum ferritin trends, therapeutic goals, and safety parameters. The 400mg tablet is often part of a regimen for patients weighing ~20kg (starting) or for dose adjustments.
Note: FOR DISPERSIBLE TABLET (common in India): Take on an empty stomach, at least 30 minutes before food. Disperse tablet completely in a glass of water, orange juice, or apple juice (100-200 mL). Stir to form a fine suspension and drink immediately. Do not chew or swallow whole. FOR FILM-COATED TABLET: Swallow whole with water on an empty stomach, at least 30 minutes before food. Take at the same time each day.
Deferasirox selectively binds ferric iron (Fe3+) with high affinity (pFe3+ = 22.5) in a 2:1 (drug:iron) ratio, forming a stable complex. This complex is then excreted primarily in the feces via biliary elimination, thereby reducing the total body iron burden and preventing iron-induced organ damage.
Pregnancy: Category D (US FDA). There is positive evidence of human fetal risk. Use only if the potential benefit justifies the potential risk to the fetus. Iron chelation is generally avoided during pregnancy unless severe iron overload is life-threatening.
Driving: May cause dizziness and visual disturbances. Patients should be cautioned about operating machinery or driving until they know how the medication affects them.
| Aluminum-containing antacids | Decreased absorption of deferasirox. Separate administration by at least 4 hours. | Moderate |
| Cholestyramine | May decrease deferasirox absorption. Avoid concomitant use. | Moderate |
| Potent UGT inducers (e.g., Rifampicin, Phenytoin, Phenobarbital, Ritonavir) | May decrease deferasirox plasma concentration, reducing efficacy. Monitor serum ferritin and consider dose increase. | Major |
| Drugs metabolized by CYP2C8 (e.g., Repaglinide, Paclitaxel) | Deferasirox may increase their plasma concentration, increasing toxicity risk. Use with caution. | Moderate |
| Drugs metabolized by CYP3A4 (e.g., Simvastatin, Midazolam) | Deferasirox may decrease their plasma concentration. Monitor efficacy. | Moderate |
| Other hepatotoxic or nephrotoxic drugs (e.g., NSAIDs, Aminoglycosides, Amphotericin B) | Increased risk of renal/hepatic toxicity. Avoid or monitor closely. | Major |
| Vitamin C (Ascorbic acid) supplements | May increase iron toxicity and tissue iron redistribution. Do not exceed 200 mg/day and monitor cardiac function. | Moderate |