Comparison of the properties of available iron chelators

	Deferoxamine	Deferasirox		Deferiprone
Administration route	Subcutaneous or intravenous	Oral		Oral
Dosage form	Solution for injection	Dispersible tablet for oral suspension (Exjade)	Film coated tablet (Jadenu) or granules to sprinkle on food (Jadenu)	Oral solution or tablet (500 mg, 1000 mg for three time-a-day use, and 1000 mg for twice-a-day use)
Usual dosage range	20 to 40 mg/kg daily, infused over 8 to 12 hours for 5 to 7 days per week. Generally administered SUBQ but may be given intravenously in cases of severe iron overload. In adults with severe cardiac iron or heart failure, up to 60 mg/kg daily may be used, infused intravenously typically over 24 hours.	Transfusional iron overload: 20 to 40 mg/kg once daily NTDT: 10 to 20 mg/kg once daily	Transfusional iron overload: 14 to 28 mg/kg once daily NTDT: 7 to 14 mg/kg once daily	75 to 99 mg/kg per day, in 2 or 3 divided doses (dose frequency depends on formulation), with at least 4 hours between doses. Only the 1000 mg twice-a-day tablet formulation should be administered in 2 divided doses.
Excretion route	Urinary (majority) and fecal	Fecal (majority) and urinary		Urinary
Efficacy for removing liver iron	+++	+++		++ Insufficient liver iron removal in some patients at doses of 70 to 75 mg/kg/day, but higher dosing may be more effective, especially with high transfusional iron burden^[1,2]
Efficacy for removing cardiac iron	++ With continuous infusion	++ One report showed less effective cardiac iron removal in patients with more severe iron loading^[3]		+++
Adverse effects (refer to UpToDate and individual drug information monographs for additional AEs)	Local reactions Ophthalmologic toxicity Audiologic toxicity Allergic reactions Bone abnormalities Increased risk of Yersinia and Klebsiella infections Pulmonary toxicity at high doses Neurologic toxicity at high doses	Retinopathy Rash Kidney toxicity (increased creatinine, proximal renal tubular dysfunction, proteinuria, rare chronic kidney disease) Elevated transaminases (rare fulminant hepatic failure) Gastrointestinal upset, bleeding/ulcers		Neutropenia and agranulocytosis Gastrointestinal upset Elevated transaminases Arthralgias Zinc deficiency
Approved uses in the United States (other countries may have other prescribing information)	Treatment of transfusional iron overload in patients with chronic anemia Not labeled for use in non-transfusion dependent anemias	Treatment of transfusional iron overload in patients ≥2 years Treatment of chronic iron overload in non-transfusion-dependent thalassemia with LIC ≥5 mg/gram dry weight and ferritin ≥300 ng/mL in patients ≥10 years		Treatment of transfusional iron overload in patients ≥8 years (tablets) or ≥3 years (oral solution) Not approved for use in non-transfusion dependent anemias

Refer to UpToDate for discussions of iron chelator selection, dosing, and adverse events.

AEs: adverse effects; LIC: liver iron concentration; NTDT: non-transfusion-dependent thalassemia; SUBQ: subcutaneously.

References:

Olivieri NF, Brittenham GM, McLaren CE, et al. Long-term safety and effectiveness of iron-chelation therapy with deferiprone for thalassemia major. N Engl J Med 1998; 339:417.
Mazza P, Amurri B, Lazzari G, et al. Oral iron chelating therapy. A single center interim report on deferiprone (L1) in thalassemia. Haematologica 1998; 83:496.
Wood JC, Kang BP, Thompson A, et al. The effect of deferasirox on cardiac iron in thalassemia major: Impact of total body iron stores. Blood 2010; 116:537.

Adapted from: Kwiatkowski JL. Management of transfusional iron overload - Differential properties and efficacy of iron chelating agents. J Blood Med 2011; 2:135.

Graphic 145611 Version 2.0

خرید پکیج

Comparison of the properties of available iron chelators