Table 1

Comparison of the main available iron chelators to an ideal chelation drug (modified from [2469])

"Ideal chelator"

Deferoxamine

Deferiprone

Deferasirox

Route of administration

Oral

Parenteral, usually subcutaneous or intravenous

Oral

Oral

Plasma half-life

Long enough to give constant protection from labile plasma iron

Short (minutes); requires constant delivery

Moderate (< 2 hours). Requires at least 3-times-per-day dosing

Long, 8–16 hours; remains in plasma at 24 h

Therapeutic index

High

High at moderate doses in iron-overloaded subjects

Idiosyncratic side effects are most important

Probably high in iron overloaded subjects*

Molar iron chelating efficiency; charge of iron (III) complex

High, uncharged

High (hexadentate); charged

Low (bidentate); uncharged

Moderate (tridentate); uncharged

Important side effects

None or only in iron-depleted subjects

Auditory and retinal toxicity; effects on bones and growth; potential lung toxicity, all at high doses; local skin reactions at infusion sites

Rare but severe agranulocytosis; mild neutropenia; common abdominal discomfort; erosive arthritis

Abdominal discomfort; rash or mild diarrhoea upon initiation of therapy; mild increased creatinine level

Ability to chelate intracellular cardiac and other tissue iron in humans

High

Probably lower than deferiprone and deferasirox (it is not clear why)

High in clinical and in in vitro studies

Insufficient clinical data available; promising in laboratory studies

*Nephrotoxicity that has been observed in non-iron-loaded animals has been minimal in iron-overloaded humans, but effectiveness is demonstrated only at higher end of tested doses, as discussed in [1693].

Kell BMC Medical Genomics 2009 2:2   doi:10.1186/1755-8794-2-2