Deferiprone (L1) Query Show help

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Tamoxifen (TAM) is a non-steroidal antiestrogen used in the treatment and prevention of hormone-dependent breast cancer. Tamoxifen therapy may be accompanied with hepatic injury and iron accumulation in this organ. The present study investigates the influence of the effective oral iron chelator, deferiprone (L1), in TAM-induced acute liver injury. Four groups of female Wistar rats were used: I, control; II, TAM; III, TAM+L1; IV, L1. Tamoxifen (75 mg/kg) was administered orally on the first and second day; L1 (50 mg/kg) was administered orally on the first, second and third day of the experiment. On the fourth day, parameters of oxidative state: lipid peroxidation (LP), glutathione (GSH) and catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) activities were estimated in liver homogenates. Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), glutamate dehydrogenase (GLDH) levels and iron hepatic content were also evaluated. The TAM-induced oxidative damage was demonstrated by increased LP (52% above controls) and decreased GPx activity (to 92% of controls). The protective effect of L1 was manifested by attenuation of LP (p <0.05) and preserving of GPx activity. The TAM-induced increase of serum ALT and AST activity remained unchanged by L1 treatment. Significant increase of hepatic iron (Fe) level (41% above controls) was found in TAM-treated rats. Hepatic Fe accumulation was completely prevented by L1 treatment.

MeSH
Iron Chelating Agents MeSH
Enzyme Assays MeSH
Rats MeSH
Chemical and Drug Induced Liver Injury drug therapy etiology metabolism MeSH
Protective Agents MeSH
Lipid Peroxidation drug effects MeSH
Rats, Wistar MeSH
Pyridones pharmacology therapeutic use MeSH
Tamoxifen adverse effects MeSH
Treatment Outcome MeSH
Iron metabolism MeSH
Animals MeSH
Check Tag
Rats MeSH
Female MeSH
Animals MeSH
Publication type
Journal Article MeSH
Research Support, Non-U.S. Gov't MeSH

Online article

Efficacy and safety of administration of oral iron chelator deferiprone in patients with early myelodysplastic syndrome

... average initial serum ferritin levels of 2739.5 μg/L (range 825-11287 μg/L), were treated with deferiprone ...

Hemoglobin. 2011 ; 35 (3) : 217-27.

ISSN 1532-432X
Medvik
Source

Forty-eight patients with early myelodysplastic syndrome (MDS) without excess of blasts, with average initial serum ferritin levels of 2739.5 μg/L (range 825-11287 μg/L), were treated with deferiprone (L1) in a daily dose of 40-90 mg/kg. Median duration of chelation treatment was 10.9 months (range 4-24 months). Chelation was effective (maintained or decreased iron stores) in 16 out of 22 patients (73%) with serum ferritin levels <2000 μg/L in contrast to only 12 out of 26 patients with serum ferritin levels >2000 μg/L. Combination of L1 with recombinant human erythropoietin (rHuEPO) (30-40 kU/week) resulted in effective chelation in five additional patients with serum ferritin levels >3000 μg/L. Incidence of adverse effects was comparable to that in thalassemic patients. Gastrointestinal symptoms represented the most frequent adverse effect of L1 therapy (37.5% of patients) that limited an effective escalation of the daily dose of the drug and led to discontinuation of the treatment for six patients. A decreased number of granulocytes was observed in five (13%) patients and agranulocytosis occurred in two patients (4%). Granulocyte counts were restored after cessation of L1 treatment and administration of granulocyte colony stimulating factor (G-CSF) in all but one patient. Administration of L1 in a daily dose of at least 75 mg/kg may represent an alternative approach in treatment of mild and moderate iron overload in MDS patients who cannot be treated with deferasirox (DFRA) or deferoxamine (DFO).