化合物信息

Drug Groups

approved; investigational

Description

Deferasirox is an oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved in the USA for this purpose.

Indication

For the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.

Pharmacology

Deferasirox is an orally active chelator that is selective for iron (as Fe3+). 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.

Affected Organisms

Biotransformation

Hepatic. CYP450-catalyzed (oxidative) metabolism of deferasirox appears to be minor in humans (about 8%). Glucuronidation is the main metabolic pathway for deferasirox, with subsequent biliary excretion.

Absorption

The absolute bioavailability (AUC) of deferasirox tablets for oral suspension is 70% compared to an intravenous dose.

Half Life

The mean elimination half-life ranged from 8 to 16 hours following oral administration.

Protein Binding

Deferasirox is highly (~99%) protein bound almost exclusively to serum albumin.

Elimination

Deferasirox and metabolites are primarily (84% of the dose) excreted in the feces.
Renal excretion of deferasirox and metabolites is minimal (8% of the administered dose).

Distribution

* 14.37 ± 2.69 L

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