Absolute oral bioavailability and disposition of deferasirox in healthy human subjects

Journal of Clinical Pharmacology

Volumn 48, Issue 8, 2008, Pages 919-925

  Séchaud, Romain ^a   Robeva, Anna ^a   Belleli, Rossella ^a   Balez, Sebastien ^b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b NOVARTIS PHARMA K K   (Japan)

Author keywords

Bioavailability; Chelation; Deferasirox; Iron overload; Pharmacokinetics

Indexed keywords

DEFERASIROX; DEFEROXAMINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISPOSITION; DRUG DISTRIBUTION; DRUG DOSAGE FORM COMPARISON; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; HUMAN EXPERIMENT; IRON OVERLOAD; MALE; MAXIMUM PLASMA CONCENTRATION; MORNING DOSAGE; NAUSEA; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADOLESCENT; ADULT; AREA UNDER CURVE; BENZOIC ACIDS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; CROSS-OVER STUDIES; DOUBLE-BLIND METHOD; HALF-LIFE; HUMANS; INFUSIONS, INTRAVENOUS; IRON CHELATING AGENTS; MALE; MIDDLE AGED; TISSUE DISTRIBUTION; TRIAZOLES;

EID: 47549099814     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270008320316     Document Type: Article

References (14)

1. Rund D., Rachmilewitz E. Beta-thalassemia. N Engl J Med. 2005 ; 353: 1135-1146.
2. Aldouri MA, Wonke B., Hoffbrand AV, et al. Iron state and hepatic disease in patients with thalassaemia major, treated with long term subcutaneous desferrioxamine. J Clin Pathol. 1987 ; 40: 1353-1359.
3. Piga A., Galanello R., Forni GL, et al. Randomized phase II trial of deferasirox (Exjade, ICL670), a once-daily, orally-administered iron chelator, in comparison to deferoxamine in thalassemia patients with transfusional iron overload. Haematologica. 2006 ; 91: 873-880.
4. Porter JB Practical management of iron overload. Br J Haematol. 2001 ; 115: 239-252.
5. Vanorden HE, Hagemann TM Deferasirox-an oral agent for chronic iron overload. Ann Pharmacother. 2006 ; 40: 1110-1117.
6. Cappellini MD, Cohen A., Piga A., et al. A phase 3 study of deferasirox (ICL670), a once-daily oral iron chelator, in patients with beta-thalassemia. Blood. 2006 ; 107: 3455-3462.
7. Galanello R., Piga A., Alberti D., et al. Safety, tolerability, and pharmacokinetics of ICL670, a new orally active iron-chelating agent in patients with transfusion-dependent iron overload due to beta-thalassemia. J Clin Pharmacol. 2003 ; 43: 565-572.
8. Nisbet-Brown E., Olivieri NF, Giardina PJ, et al. Effectiveness and safety of ICL670 in iron-loaded patients with thalassaemia: a randomised, double-blind, placebo-controlled, dose-escalation trial. Lancet. 2003 ; 361: 1597-1602.
9. Robinett-Weiss N., Hixson ML, Keir B., et al. The Metropolitan height-weight tables: perspectives for use. J Am Diet Assoc. 1984 ; 84: 1480-1481.
10. Galanello R., Piga A., Cappellini MD, et al. Effect of food, type of food, and time of food intake on deferasirox bioavailability: recommendations for an optimal deferasirox administration regimen. J Clin Pharmacol. 2008 ; 48: 428-435.
11. Roberts MS, Magnusson BM, Burczynski FJ, et al. Enterohepatic circulation: physiological, pharmacokinetic and clinical implications. Clin Pharmacokinet. 2002 ; 41 (10). 790.
12. Weiss HM, Fresneau M., Camenisch GP, Kretz O., Gross G. In vitro blood distribution and plasma protein binding of the iron chelator deferasirox (ICL670) and its iron complex Fe-[ICL670]2 for rat, marmoset, rabbit, mouse, dog, and human. Drug Metab Dispos. 2006 ; 34 (6). 971-975.
13. Nick H., Wong A., Acklin P., et al. ICL670A: preclinical profile. Adv Exp Med Biol. 2002 ; 509: 185-203.
14. Breur W., Hershko C., Cabantchik ZI The importance of nontransferrin bound iron in disorders of iron metabolism. Transfus Sci. 2000 ; 23: 185-192.