Reference

Deferasirox: an effective once-daily orally active iron chelator

All Rights Reserved. Deferasirox: an effective once-daily orally active iron chelator. Porter, John B. (Head of Thalassaemia and Sickle Unit, University College London Hospitals, University College of London, UK). Drugs of Today, 42(10), 623-637 (English) 2006 Prous Science. CODEN: MDACAP. ISSN: 1699-3993. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. Deferasirox (ICL670) in an orally absorbed tridentate chelator of iron (III), intended as a once-daily monotherapy for transfusional iron overload. Deferasirox was identified by Novartis from over 700 mol.Several reagents with their cas registry numbers 7439-89-6 and 201530-41-8 are used here. entities in preclin. screening, comparing favorably with parenteral desferrioxamine or oral deferiprone. Clin. phase I and II studies demonstrated an exclusively fecal route of iron excretion, with a long plasma half-life, suitable for once-daily dosing and 24-h protection from labile iron. Systematic large-scale prospective clin. trials have been completed in thalassemia major, sickle cell disease, and other transfusionally dependent anemias, such as myelodysplastic syndrome. These show dose-dependent redn. in body iron and have identified doses necessary either to stabilize or to decrease iron loading according to transfusion requirements. Tolerability after more than two years in phase III studies is good, with a low trial dropout rate and no drug-related arthropathy or agranulocytosis. An early, nonprogressive serum creatinine increase, remaining within normal ranges, was seen in about one-third of patients. Preliminary clin. findings using T2* as well as preclin. models suggest good drug access to myocardial iron. Deferasirox is currently registered as monotherapy for transfusional iron overload in more than 65 countries worldwide, including the United States and in the European Union. .

Deferasirox-an oral agent for chronic iron overload

All Rights Reserved. Deferasirox-an oral agent for chronic iron overload.Several substances are used for example 7439-89-6 and 201530-41-8 which are their cas registry numbers. VanOrden, Heidi E.; Hagemann, Tracy M. (Center for Cancer and Blood Disorders, Children's Medical Center of Dallas, Dallas, TX, USA). Annals of Pharmacotherapy, 40(6), 1110-1117 (English) 2006 Harvey Whitney Books Co. CODEN: APHRER. ISSN: 1060-0280. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) Objective: To review the available literature on the pharmacol., pharmacokinetics, efficacy, toxicol., adverse effects, drug interactions, and dosage guidelines for deferasirox, an oral iron chelator, in Phase III trials. Data Sources: Reviewers searched the following databases for English-language studies: MEDLINE (1966-Apr. 2006), International Pharmaceutical Abstrs. (1970-Apr. 2006), and the Cochrane Library Database. Key search terms included iron chelation, chelation, iron overload, deferasirox, and ICL670. Study Selection And Data Extn.: Data on efficacy, toxicol., adverse effects, and pharmacokinetics for deferasirox were obtained from randomized, open-label, blinded clin. trials. Other information was obtained from the manufacturer, including unpublished studies in abstr. form as well as available data on deferasirox. Data Synthesis: Deferasirox is an orally active iron chelator. In clin. trials, deferasirox demonstrated efficacy at dosages of 20 and 30 mg/kg/day in treating iron overload in patients with b-thalassemia. Deferasirox has been studied in patients older than 2 years and appears to be safe, with the most common adverse effects reported being mild, transient nausea, gastrointestinal disturbances, and rash. There were no reports of serious adverse effects in trials to date. Conclusions: Deferasirox represents a new approach to the management of chronic iron overload in patients with chronic anemias who require blood transfusions. The available literature suggests that deferasirox is safe and as effective as the current std. of therapy at dosages of 20-30 mg/kg/day for b-thalassemia. Further studies are needed to confirm its efficacy in other chronic transfusion-requiring diseases. .