DEFRATAJ (Deferasirox) - Master Product Reference

DEFRATAJ is Taj Pharma's branded generic of Deferasirox, an orally active, tridentate iron chelator indicated for chronic transfusional iron overload. Available as a dispersible tablet in five strengths (100, 125, 250, 400, 500 mg) for accurate weight-based once-daily dosing in adult and pediatric patients.

Iron overload arises when repeated red-cell transfusions deliver iron faster than the body can excrete it (each unit contains roughly 200 mg of elemental iron). Without effective chelation, this iron deposits in liver, heart, pancreas and pituitary, driving cirrhosis, cardiomyopathy and endocrine failure.

Deferasirox is a tridentate iron chelator: each molecule provides three coordination atoms (one phenolate oxygen, two triazole nitrogens). Two molecules wrap around one Fe3+ in a 2:1 ligand-to-metal ratio, forming a neutral, redox-inactive hexacoordinate complex. The drug is highly protein-bound (~99%), allowing interception of labile plasma iron and non-transferrin-bound iron. The deferasirox-iron complex is taken up by the liver and excreted into bile. Selectivity for Fe3+ over essential trace metals (Zn, Cu) supports long-term safety.

Inside the body, iron from blood transfusions can build up over time and damage organs such as the liver and heart. DEFRATAJ helps the body remove this extra iron safely. Once a tablet is swallowed (after dispersing it in water or juice), the medicine travels in the blood, latches onto excess iron, and the iron-medicine pair leaves the body mainly in stool through bile. Taken once a day, it works around the clock to keep iron levels under control.

DEFRATAJ is indicated for the treatment of chronic iron overload due to frequent blood transfusions in patients with:

• Beta-thalassemia major
• Sickle-cell disease and other transfusion-dependent anemias
• Myelodysplastic syndromes (MDS)
• Other rare anemias requiring regular transfusion support (where locally approved)

Locally approved indications, age limits and transfusion-burden thresholds vary by market and should be checked against the prescribing information registered with the relevant national authority.

Once-Daily Dosing

Administered once daily, on an empty stomach, at least 30 minutes before food, at the same time each day.

Weight-Based Dosing

Calculated on a mg/kg basis. Typical starting doses for transfusion-dependent iron overload are around 20 mg/kg/day with the dispersible formulation, adjusted in 5-10 mg/kg increments every 3-6 months based on serum ferritin trends and tolerability. Always refer to locally approved prescribing information.

Step-by-Step Dispersible Usage

1. Drop the tablet(s) into 100-200 ml of water, orange juice or apple juice.
2. Stir until fully dispersed into a fine suspension.
3. Drink the entire suspension immediately.
4. Rinse the glass with a small additional volume and drink that as well.
5. Take on an empty stomach, 30 minutes before food, same time daily.

Monitoring & Adjustment

Serum ferritin monthly. Renal function (creatinine, CrCl) and liver function tests before initiation and at regular intervals during treatment. Doses adjusted based on iron-burden trend, tolerability and laboratory monitoring.

Common Adverse Reactions

• GI: nausea, vomiting, diarrhoea, abdominal pain
• Skin: rash (mild to moderate)
• Lab: rises in serum creatinine and liver enzymes (often dose-related and reversible)

Serious Adverse Reactions

• Renal: acute renal failure, including fatal cases - particularly in elderly or volume-depleted patients
• Hepatic: hepatic dysfunction, including hepatic failure
• Cytopenias (agranulocytosis, neutropenia, thrombocytopenia) - predominantly in MDS patients with pre-existing risk
• GI haemorrhage and ulceration, particularly in elderly patients

Severe Cutaneous Adverse Reactions (SCAR)

• Hypersensitivity to deferasirox or any excipient
• Estimated creatinine clearance < 60 mL/min (refer to locally approved label)
• High-risk MDS or advanced malignancy where benefit-risk is unfavourable
• Combination with other iron-chelation therapies, unless under specialist supervision

• Aluminium-containing antacids: avoid simultaneous administration; deferasirox can chelate aluminium.
• UGT inducers (rifampicin, phenytoin, phenobarbital, ritonavir): may decrease deferasirox exposure - monitor ferritin and adjust dose.
• CYP3A4 substrates (ciclosporin, simvastatin, hormonal contraceptives): deferasirox can reduce exposure - clinical monitoring recommended.
• CYP1A2 substrates with narrow therapeutic index (theophylline): caution and therapeutic monitoring advised.
• Bile-acid sequestrants: may reduce efficacy.

Paediatric Use

Approved for pediatric transfusion-dependent iron overload from age 2 years (transfusional) and 6 years (non-transfusional thalassemia) in many markets. Growth and sexual development should be monitored.

Geriatric Use

Elderly patients are at higher risk of GI haemorrhage, renal impairment and cytopenias - close monitoring required.

Hepatic Impairment

Avoid in severe hepatic impairment (Child-Pugh C). Use with caution and dose reduction in moderate hepatic impairment.

Renal Impairment

Contraindicated when CrCl < 60 mL/min. Discontinue if creatinine rises persistently above ULN. Monitor renal function before and during treatment.

Limited overdose data. Single doses up to 80 mg/kg in iron-overloaded thalassaemic patients have been tolerated with mild nausea and diarrhoea. There is no specific antidote. Management is supportive: monitor renal and hepatic function, treat symptomatically. Dialysis is not expected to be effective due to high protein binding.

Store below 30 degrees C. Protect from moisture. Keep in the original blister/container. Keep out of reach of children. Do not use after the expiry date stated on the carton.

Unused or expired DEFRATAJ should be disposed of in accordance with local regulations for pharmaceutical waste. Do not dispose of medicines via wastewater or household refuse. Patients should return unused tablets to a pharmacy or designated collection point. Healthcare facilities should follow biomedical-waste handling standards applicable in their jurisdiction.