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Chelators for treatment of iron and copper overload: Shift from low-molecular-weight compounds to polymers

Hruby, M.; Santana Martinez, I. I.; Stephan, H.; Pouckova, P.; Benes, J.; Stepanek, P.


Iron and copper are essential micronutrients needed for the proper function of every cell. However, in excessive amounts these elements are toxic as they may cause oxidative stress resulting in damage of liver and other organs. This may happen due to poisoning, as side effect of thalassemia infusion thera-py or due to hereditary diseases hemochromatosis or Wilson´s disease. The current golden standard of therapy of iron and copper overload is the use of low-molecular-weight chelators of these elements. However, these agents suffer from severe side effects, are often expensive and possess unfavourable pharmacokinetics, which is all limiting useability of such therapy. The emerging concept are poly-mer-supported iron- and copper-chelating therapeutics, either for parenteral or oral use, which show vivid potential to keep therapeutic efficacy of low-molecular-weight agents while avoiding their draw-backs and especially side effects. Critical evaluation of this new perspective polymer approach is the purpose of this review article.

Keywords: iron; copper; polymer; chelator; Wilson's disease; hemochromatosis


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