Deferasirox pharmacokinetic evaluation in β‐thalassaemia paediatric patients. (27th May 2016)

• Record Type: Journal Article
• Authors: Allegra, Sarah; Cusato, Jessica; De Francia, Silvia; Pirro, Elisa; Massano, Davide; Piga, Antonio; D'Avolio, Antonio
• Other Names: Tuleu Catherine guestEditor.
• Is Part Of: Journal of pharmacy and pharmacology. Volume 69:Number 5(2017:May)
• Page Start: 525
• Page End: 528
• Publication Date: 2016-05-27
• Subjects: AUC -- iron chelator -- iron overload -- β‐thalassaemia -- transfusion; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12559
• Languages: English
• ISSNs: 0022-3573

Abstract

Abstract: Objectives: Iron chelation in the transfusion‐dependent anaemias management is essential to prevent end‐organ damage and to improve survival. Deferasirox is a once‐daily orally active tridentate selective iron chelator which pharmacokinetic disposition could influence treatment efficacy and toxicity. Therapeutic drug monitoring is an important tool for optimizing drug utilization and doses. Methods: A fully validated chromatographic method was used to quantify deferasirox concentration in plasma collected from paediatric patients with β‐thalassaemia. Samples obtained after 5 days of washout or in naïve patients before and after 2, 4, 6 and 24 h drug administration were evaluated. Key findings: Associations between variables were tested using the Pearson test. Twenty paediatric patients were enrolled; they were mainly men (13.65%), with median age of 6.35 years and body mass index of 15.45 kg/m 2 . Concerning pharmacokinetic parameters, a higher interindividual variability was shown. A positive, but not significant, correlation ( r = 0.363; P = 0.115) was found between deferasirox area under the concentration curve over 24 h (AUC) and drug dose. Conclusions: Monitoring plasma deferasirox concentrations appears beneficial for guiding appropriate patient treatment, enhancing effectiveness and minimizing toxicity.