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Chemists modify drug to improve treatment of metal overload conditions

The research was featured on the front cover of the journal ChemMedChem

An international team of chemists have modified and improved upon a drug used to treat metal overload conditions.

This may lead to better treatment of chronic iron overload, often experienced by patients receiving long-term blood transfusions, as well as other conditions.

Metal overload can be caused by imbalances as a result of genetic diseases or through over-exposure. The health implications can be severe and chelation therapy is considered as one treatment option to decrease the toxic effects of metal overload in the human body.

The team of chemists, including Dr Andrew McGown, a Research Fellow based in the Spencer Lab, modified a known chelation drug – Deferasirox – by combining it with another type of chemical: a Cyclodextrin.

John Spencer, Professor of Bioorganic Chemistry and lead author of the research, said: “This new type of drug-like entity displays improved biological properties, making it less toxic than the currently used and FDA approved drug Deferasirox.

“Our new Cyclodextrin-Deferasirox hybrid may be more effective in treating metal overloads such as chronic iron overload in patients receiving long-term blood transfusions. It also shows great promise in treating Niemann Pick C, a rare genetic disease characterised by lipid and metal imbalances in cells.”

The paper, Synthesis and Study of Novel Multifunctional Cyclodextrin-Deferasirox Hybrids, is published in ChemMedChem.

The international study was funded by the Wellcome Trust, Università degli Studi di Catania, the Italian Ministero dell’Università e della Ricerca and the Niemann Pick Research Foundation and involved partners from Eurofins Drug Discovery, Oxford, Kings College and Catania Universities.

By: Jessica Gowers
Last updated: Wednesday, 21 August 2019