The first iron chelator to treat iron overload, desferrioxamine, was developed in the 1960’s. It is known as a siderophore, which are molecules secreted by bacteria to gather atoms of iron from their surroundings for use in various metabolic pathways. Desferrioxamine is a very large molecule and because of its chemical and physical properties it cannot be taken orally because it is poorly absorbed and broken down quickly in the digestive system. It has to be administered by injection, usually by a subcutaneous infusion via a portable pump. Because desferrioxamine has a short half-life in the circulatory system, its infusions are given over 8 -12 hours for 5 - 7 days each week to effectively remove iron from the body.

After many years of intensive research, an iron chelator that was orally active, deferiprone, was first used in men in 1987 in the United Kingdom (Kontoghiorghes, 1987). In 1993 Apotex acquired the worldwide rights to develop deferiprone as an oral iron chelator and it was given the name Ferriprox. Following the clinical trials to determine the safety and efficacy of Ferriprox, it was approved in the 15 countries of the European Union (Austria, Germany, Netherlands, Luxembourg, Italy, Greece, Spain, France, Sweden, Denmark, Finland, Belgium, Portugal, United Kingdom, and Ireland) in August 1999. Today, 54 countries have approved Ferriprox® for the treatment of iron overload. For more information on Ferriprox® check the section About Ferrirpox®.

A third iron chelator, deferasirox, is now available in certain markets. Deferasirox is an oral iron chelator that is dissolved in water or juice and is taken once daily.