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Table 1 Comparison of the main available iron chelators to an ideal chelation drug (modified from 2469)

From: Iron behaving badly: inappropriate iron chelation as a major contributor to the aetiology of vascular and other progressive inflammatory and degenerative diseases

  "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
  1. *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.