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 Metabolism and Disposition

Volumn 34, Issue 6, 2006, Pages 971-975

  Weiss, H Markus ^a   Fresneau, Marcel ^a   Camenisch, Gian P ^a   Kretz, Olivier ^a   Gross, Gerhard ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

BIOLOGICAL MARKER; CHELATING AGENT; DEFERASIROX; DIAZEPAM; IRON BINDING PROTEIN; IRON COMPLEX; PLASMA PROTEIN; SERUM ALBUMIN; WARFARIN;

ARTICLE; BLOOD LEVEL; CONTROLLED STUDY; DOG; DRUG BINDING SITE; DRUG DISTRIBUTION; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG STRUCTURE; FEMALE; HUMAN; IN VITRO STUDY; IRON BLOOD LEVEL; MALE; MARMOSET; MOUSE; NONHUMAN; NORMAL HUMAN; PLASMA PROTEIN BINDING; PLASMA VOLUME; PRIORITY JOURNAL; PROTEIN ISOLATION; RABBIT; RAT; SPECIES COMPARISON;

ANIMALS; BENZOIC ACIDS; BINDING, COMPETITIVE; CALLITHRIX; DIAZEPAM; DOGS; FEMALE; FERROUS COMPOUNDS; HUMANS; IRON CHELATING AGENTS; MALE; MICE; PROTEIN BINDING; RABBITS; RATS; SERUM ALBUMIN; TRIAZOLES; WARFARIN;

CANIS FAMILIARIS; MARMOSETS; ORYCTOLAGUS CUNICULUS;

EID: 33646809736     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.006429     Document Type: Article

References (14)

1. Benet LZ and Hoener BA (2002) Changes in plasma protein binding have little clinical relevance. Clin Pharmacol Ther 71:115-121.
2. Chen J and Hage DS (2004) Quantitative analysis of allosteric drug-protein binding by biointeraction chromatography. Nat Biotechnol 22:1445-1448.
3. Crichton RR and Ward RJ (2003) An overview of iron metabolism: molecular and cellular criteria for the selection of iron chelators. Curr Med Chem 10:997-1004.
4. Galanello R, Piga A, Alberti D, Rouan MC, Bigler H, and Sechaud R (2003) 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 43:565-572.
5. Ghuman J, Zunszain PA, Petitpas I, Bhattacharya AA, Otagiri M, and Curry S (2005) Structural basis of the drug-binding specificity of human serum albumin. J Mol Biol 353:38-52.
6. Hershko C, Link G, and Cabantchik I (1998) Pathophysiology of iron overload. Ann NY Acad Sci 850:191-201.
7. Hinderling PH (1997) Red blood cells: a neglected compartment in pharmacokinetics and pharmacodynamics. Pharmacol Rev 49:279-295.
8. Nick H, Acklin P, Lattmann R, Buehlmayer P, Hauffe S, Schupp J, and Alberti D (2003) Development of tridentate iron chelators: from desferrithiocin to ICL670. Curr Med Chem 10:1065-1076.
9. Nisbet-Brown E, Olivieri NF, Giardina PJ, Grady RW, Neufeld EJ, Sechaud R, Krebs-Brown AJ, Anderson JR, Alberti D, Sizer KC, et al. (2003) Effectiveness and safety of ICL670 in iron-loaded patients with thalassaemia: a randomised, double-blind, placebo-controlled, doseescalation trial. Lancet 361:1597-1602.
10. Porter JB (2001) Deferoxamine pharmacokinetics. Semin Hematol 38:63-68.
11. Rolan PE (1994) Plasma protein binding displacement interactions - why are they still regarded as clinically important? Br J Clin Pharmacol 37:125-128.
12. Sansom LN and Evans AM (1995) What is the true clinical significance of plasma protein binding displacement interactions? Drug Saf 12:227-233.
13. Steinhauser S, Heinz U, Bartholoma M, Weyhermueller T, Nick H, and Hegetschweiler K (2004) Complex formation of ICL670 and related ligands with Fe(III) and Fe(II). Eur J Inorg Chem 2004:4177-4192.
14. Sudlow G, Birkett DJ, and Wade DN (1976) Further characterization of specific drug binding sites on human serum albumin. Mol Pharmacol 12:1052-1061.