Pharmacology: Pharmacodynamics: Deferasirox selectively binds iron, forming a complex that is excreted primarily through the feces.
Pharmacokinetics: Absorption: Deferasirox is well absorbed following oral administration, with peak plasma concentrations usually attained within 1.5 - 4 hours. The absolute oral bioavailability of the drug is 70%. Food variably increases the bioavailability of Deferasirox.
Distribution: Deferasirox volume distribution in adults is 14.4 ± 2.7 Liters. Protein binding is approximately 99% to serum albumin.
Metabolism: Deferasirox is metabolized principally in the liver via glucuronidation by uridine diphosphate-glucuronosyltransferase (UGT1A1) and to a lesser extent by UGT1A3. Deferasirox is minimally metabolized (8%) by oxidative cytochrome P-450 (CYP) enzymes. Deferasirox undergoes enterohepatic recirculation.
Excretion: Deferasirox and its metabolites are eliminated principally in feces via bile (84%) and to a lesser extent in urine (8%). The half-life of Deferasirox is 7-16 hours.