Deferasirox

What it is and how it works

Mechanism of Action Deferasirox tablets for oral suspension are an orally active chelator that is selective for iron (as Fe 3+ ). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain.

Mechanism class: Iron Chelating Activity · Cytochrome P450 3A4 Inducers · Cytochrome P450 2C8 Inhibitors

Indications

Deferasirox tablets for oral suspension are an iron chelator indicated for the treatment of chronic iron overload due to blood transfusions in patients 2 years of age and older. Deferasirox tablets for oral suspension is indicated for the treatment of chronic iron overload in patients 10 years of age and older with non-transfusion-dependent thalassemia (NTDT) syndromes, and with a liver iron (Fe) concentration (LIC) of at least 5 mg Fe per gram of dry weight and a serum ferritin greater than 300 mcg/L. Limitations of Use: The safety and efficacy of deferasirox tablets for oral suspension when administered with other iron chelation therapy have not been established. Treatment of Chronic Iron Overload Due to Blood Transfusions (Transfusional Iron Overload) Deferasirox tablets for oral suspension are indicated for the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.

Dosage and administration (summary)

Transfusional Iron Overload: Initial dose for patients with estimated glomerular filtration rate (eGFR) greater than 60 mL/min/1.73 m 2 is 20 mg per kg body weight once daily, as oral suspension. Calculate dose to the nearest whole tablet. NTDT Syndromes: Initial dose for patients with eGFR greater than 60 mL/min/1.73 m 2 is 10 mg per kg body weight once daily, as oral suspension. Calculate dose to the nearest whole tablet. Transfusional Iron Overload Deferasirox tablets for oral suspension therapy should only be considered when a patient has evidence of chronic transfusional iron overload.

Contraindications

Deferasirox tablets for oral suspension are contraindicated in patients with: Estimated GFR less than 40 mL/min/1.73 m 2 ; Poor performance status; High-risk myelodysplastic syndromes; (this patient population was not studied and is not expected to benefit from chelation therapy) Advanced malignancies. Platelet counts less than 50 x 10 9 /L Known hypersensitivity to deferasirox or any component of deferasirox tablets for oral suspension . • Estimated GFR less than 40 mL/min/1.73 m 2 .

Warnings and precautions

Acute Kidney Injury: Measure serum creatinine in duplicate before starting therapy. Monitor renal function during deferasirox tablets for oral suspension therapy and reduce dose or interrupt therapy for toxicity. (2.1, 2.4, 5.1) Hepatic Toxicity: Monitor hepatic function. Reduce dose or interrupt therapy for toxicity. Fatal and Nonfatal Gastrointestinal Bleeding, Ulceration, and Irritation: Risk may be greater in patients who are taking deferasirox tablets for oral suspension in combination with drugs that have known ulcerogenic or hemorrhagic potential.

Pregnancy

Pregnancy Risk Summary There are no studies with deferasirox tablets for oral suspension in pregnant women to inform drug-associated risks. Administration of deferasirox to rats during pregnancy resulted in decreased offspring viability and an increase in renal anomalies in male offspring at doses that were about or less than the recommended human …

Storage and supply

Deferasirox Tablets for Oral Suspension 125 mg White to off-white, round, flat tablets debossed with “L461” on one side and plain on the other side. NDC 62332-324-30 Bottle of 30 tablets Deferasirox Tablets for Oral Suspension 250 mg White to off-white, round, flat tablets debossed with “L462” on one side and plain on the other side.

Source: Deferasirox (Deferasirox) — US FDA prescribing information, 2023-03-16, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.