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地拉罗司是一种什么药物呢?

Author: Medicalhalo
Release time: 2025-10-19 11:44:20

(DFS, ICL670), deferasirox is currently the only oral iron chelator developed by Novartis. The pharmacokinetics of deferasirox were studied. Five adult patients with thalassemia took 20 mg of deferasirox orally daily. After 7 days, the pharmacokinetics reached a stable state. Blood, plasma, feces, and urine samples were collected to analyze the concentrations of radioactive deferasirox, Fe-deferasirox complex, and deferasirox metabolites, and study the absorption, distribution, metabolism, and excretion processes of deferasirox. Studies have shown that deferasirox is well absorbed, with radioactive deferasirox and its Fe complex accounting for 87% and 10% of plasma concentrations, respectively, and most of them are excreted in the feces (84%), of which 60% is radioactive deferasirox. Unaltered deferasirox in the feces is partly due to incomplete intestinal absorption and partly due to hepatobiliary elimination of deferasirox and its glucuronide (including first-pass elimination), with renal excretion of only 8%, the main component being glucuronide M6. CYP450 enzymes catalyze deferasirox, and the products are M1 (5-OH deferasirox) (CYP1A) and M4 (5-OH deferasirox) (CYP2D6). Their contents are very small, accounting for only 6% and 2%. Direct and indirect results show that the main metabolic pathway of deferasirox is through glucuronidation to generate the metabolites M3 (acyl glucuronide) and M6 (2-O-glucuronide).

Deferasirox was approved by the FDA in November 2005 for use in patients 2 years of age and older with chronic iron overload caused by blood transfusions. In December 2012, Deferasirox was approved by the European Commission for the treatment of chronic iron overload in patients aged 10 years and older with non-transfusion-dependent thalassemia (NTDT) syndrome who require chelation therapy due to contraindications or insufficiency of deferoxamine mesylate therapy. On January 23, 2013, the FDA approved a new indication for deferasirox for the treatment of chronic iron overload in patients aged 10 years and older with non-transfusion-dependent thalassemia (NTDT).

The recommended starting daily dose is 20 mg/kg. For patients who receive monthly transfusions of more than 14 mL/kg of packed red blood cells (i.e., more than 4 units/month in adults) and who need to reduce excess iron exposure, a starting dose of 30 mg/kg/day may be considered. For patients who receive monthly transfusions of less than 7 mL/kg of packed red blood cells (i.e., less than 2 units/month in adults) and who need to maintain body iron balance, a starting dose of 10 mg/kg/day may be considered.

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