RCSI discovery could copperfasten drug for new bowel cancer treatments

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Sudipto Das

RCSI research has found that a drug that is already showing promise to tackle blood cancers could potentially also be applied to treat other cancers too, if it has a small chemical tweak that includes the addition of copper.

Belinostat is an FDA-approved drug that has shown promising efficacy in blood cancers, but the drug is broken down quickly in the body, meaning it is difficult to target belinostat to solid tumours such as bowel cancers.

To overcome this limitation of belinostat, RCSI researchers designed and created a version they call copper-belinostat or “Cubisbel”, by adding copper to the drug’s chemical structure. The presence of the copper means the body is slower to break the drug down, meaning it can last longer in the body and potentially reach cancers at further sites.

To put it to the test, the researchers applied the new, copper-fastened version of the drug to bowel cancer cells and three-dimensional ‘organoids’ growing in the lab and found that it had similar anti-cancer activity compared to the belinostat with no copper added. Their experiments, described in the journal Cellular Oncology, also suggest that Cubisbel could work well in tandem with other drugs to treat bowel cancer.

“We showed that chemically modifying an FDA-approved drug for blood cancer prevents it from breaking down too quickly and provides the drug with increased potential to kill bowel cancer cells,” said researcher Dr Sudipto Das, Lecturer and Principal Investigator at RCSI School of Pharmacy and Biomolecular Sciences.

“We hope that these results will provide a basis for revisiting the potential value of this class of drugs for solid tumour cancers, such as bowel cancer, and will ultimately provide additional treatment options for cancer patients.”

The research was conducted in collaboration with Professor Celine Marmion, RCSI Department of Chemistry, with external collaborators on the study including researchers from Pennsylvania State University, University College Dublin, GeneXplain GMbH, Germany (enterprise partner) and Albert Einstein Cancer Center in New York. 

The open-access paper ‘Complexation of histone deacetylase inhibitor belinostat to Cu(II) prevents premature metabolic inactivation in vitro and demonstrates potent anti-cancer activity in vitro and ex vivo in colon cancer’ is published in Cellular Oncology.

This research was supported by grants from the Irish Research Council, Science Foundation Ireland, ERASMUS funding and EU Horizon 2020.