Iron chelation, quo vadis?

Orally bioavailable chelators for transfusional iron overload have been sought since the introduction of deferoxamine (Desferal®) in 1962. Despite tremendous efforts, to date, only deferiprone (Ferriprox®) and deferasirox (Exjade®) have successfully reached the market, reflecting the difficulty to combine oral activity and safety. Owing to the risk of failure, few new oral chelators can be expected in the future for the treatment of transfusional iron overload. As iron is involved in many disease processes, deferiprone and deferasirox have been proposed to be potentially useful in a variety of indications not characterized by general iron overload. Although it may be possible to obtain clinical benefit from current compounds, more selective chelators tailored to the particular target are needed for successful intervention in these indications.