The first successful therapeutic iron chelator was desferrioxamine which was introduced in the late 1960’s by Ciba (now
Novartis). Desferrioxamine has been an extremely successful compound having received the MMW “Pharmaceutical of the year” award
for 1991. It is a life saving and a life – prolonging drug which improves the quality of life. However it is not orally active and its
administration is both uncomfortable and expensive.
Over the past twenty years there has been a growing interest in the orally active iron chelators, deferiprone and exjade, both having been
extensively studied. The ability of these compounds to mobilize iron from the heart and endocrine tissue has presented the clinician with
some advantages over desferrioxamine. Other orally active iron chelators are currently under development and one, FBS0701 is in
The critical features necessary for the design of therapeutically useful iron chelators is presented in this review, together with recent
studies devoted to the design of such chelators. This newly emerging range of iron chelators will enable clinicians to apply iron chelation
methodology to other disease states and to begin to design personalised chelation regimes.