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 clinical trial. 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.