HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS		QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:
Sign In to gain access to subscriptions and/or personal tools.

This Article Full Text Full Text (PDF) All Versions of this Article: 0091270008320316v1 48/8/919    most recent Alert me when this article is cited Alert me if a correction is posted Citation Map Services Email this article to a friend Similar articles in this journal Similar articles in Web of Science Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Request Permissions Request Reprints Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Séchaud, R. Articles by Balez, S. Search for Related Content PubMed PubMed Citation Articles by Séchaud, R. Articles by Balez, S. Social Bookmarking                         What's this?

Absolute Oral Bioavailability and Disposition of Deferasirox in Healthy Human Subjects

From Novartis Pharma AG, Basel, Switzerland (Dr Séchaud, Ms Belleli); Novartis Pharmaceuticals, East Hanover, New Jersey (Ms Robeva); and Novartis Pharma SAS, Rueil Malmaison, France (Dr Balez).

Deferasirox is a novel iron chelator formulated as tablets for dispersion (suspension) for once-a-day oral administration. The current study evaluated the absolute bioavailability of a single 375-mg oral dose of deferasirox administered in the form of tablets compared with a 130-mg intravenous infusion of deferasirox. Since this was a first-in-man study using the deferasirox intravenous (IV) formulation, the safety and tolerability of the IV formulation was evaluated in a pilot phase with a lower dose (65 mg) in 3 subjects prior to the main phase. The main study phase consisted of 17 healthy male volunteers. Plasma concentrations of deferasirox were measured following each treatment, and pharmacokinetic parameters including absolute oral bioavailability were determined. Absolute oral bioavailability of the deferasirox tablets was 70% (90% confidence interval, 62%-80%). Deferasirox was characterized as having a low plasma clearance of 3.53 (± 0.87) L/h. A small volume of distribution of deferasirox at steady state (V_ss) of 14.37 (±2.69 L) was determined, indicating a low tissue distribution.

Key Words: Iron overload • chelation • bioavailability • deferasirox • pharmacokinetics

Address for reprints: Dr Romain Séchaud, Novartis Pharma AG, Exploratory Development, WSJ-210.4.020, CH-4002 Basel, Switzerland.

CiteULike    Complore    Connotea    Del.icio.us    Digg    Reddit    Technorati    Twitter    What's this?

This article has been cited by other articles:

				A. Skerjanec, J. Wang, K. Maren, and L. Rojkjaer Investigation of the Pharmacokinetic Interactions of Deferasirox, a Once-Daily Oral Iron Chelator, With Midazolam, Rifampin, and Repaglinide in Healthy Volunteers J. Clin. Pharmacol., February 1, 2010; 50(2): 205 - 213. [Abstract] [Full Text] [PDF]

				N. Papadopoulos, A. Vasiliki, G. Aloizos, P. Tapinis, and A. Kikilas Hyperchloremic Metabolic Acidosis Due to Deferasirox in a Patient with Beta Thalassemia Major Ann. Pharmacother., January 1, 2010; 44(1): 219 - 221. [Abstract] [Full Text] [PDF]

				D. Chirnomas, A. L. Smith, J. Braunstein, Y. Finkelstein, L. Pereira, A. K. Bergmann, F. D. Grant, C. Paley, M. Shannon, and E. J. Neufeld Deferasirox pharmacokinetics in patients with adequate versus inadequate response Blood, November 5, 2009; 114(19): 4009 - 4013. [Abstract] [Full Text] [PDF]