Objective: Many patients with transfusional iron overload are at risk for progressive organ dysfunction and early death. Poor compliance with iron chelators is believed to be a major contributing factor. The aim of this study is to evaluate the efficacy of deferasirox in comparison with deferoxamine for the treatment of transfusional iron overload in patients with β-thalassemia major. Patients and Methods: The prospective study was designed to evaluate once-daily deferasirox for 48 weeks in forty patients ≥2 years with β-thalassaemia major with iron overload who were previously either had no chelating agent or chelated with deferoxamine. Most patients began treatment with deferasirox 10 mg⁄ kg ⁄ day and may be increased to 30 mg/kg /day. Serum ferritin level was assessed before and after beginning of deferasirox (Exjade) treatment at 3 months interval for 48 weeks. Results: Adverse events most commonly associated with deferasirox were mild, including transient nausea, vomiting, diarrhea, abdominal pain and skin rash. The mean serum ferritin level had significantly decreased in all β-thalassaemia major patients with iron overload treated with deferasirox compared to those on deferoxamine. Conclusion Administration of Exjade therapy as an oral drug is considered to be preferable and effective than the parenteral iron chelating therapy due to the poor patient compliance and poor practical regimen of parenteral infusions.