Ceritinib drug can treat patients with ALK-rearranged non-small cell lung cancer. Ceritinib has anti-cancer acivity and can be used in treating other cancers as well.

‘Ceritinib used in treating ALK-rearranged non-small cell lung cancer can also treat other cancers, and when combined with paclitaxel drug can be more effective.’

A team of researchers at Moffitt Cancer Center used cellular drug screening, functional proteomics and computer-based modeling to determine whether drugs with well-known targets may be repurposed for use against other biological targets. 




The research team found that ceritinib has anti-cancer activity against previously unknown targets. Their results were published in the journal, Nature Chemical Biology.
For the past 20 years, there has been an emphasis on targeted cancer therapy targeting a specific driver of cancer development to minimize side effects typically seen with chemotherapy. This personalized approach has been successful in certain types of cancer that are primarily driven by a single DNA alteration, such as found in chronic myeloid leukemia. However, the majority of cancers are not caused by a single mutation; rather, cancer is more commonly caused by a large network of mutations and alterations.
Some researchers, including those from Moffitt, are beginning to rethink the targeted approach to cancer therapy. They believe that developing drugs that act on multiple targets, called a polypharmacology approach, may more effectively treat those cancers that have a network of alterations.
In order to identify drugs that act on multiple targets, Moffitt researchers screened 240 drugs that are either FDA approved or in clinical development. They noticed that the drug ceritinib acts differently than other drugs in its class.
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After an extensive set of experiments to learn how ceritinib worked in cells without ALK rearrangements, they discovered the drug inhibits several other previously unknown targets, and that these signals converge onto a protein known to be responsible for causing drug resistance to paclitaxel.
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These findings suggest that ceritinib together with paclitaxel may be effective against other cancers that do not have ALK rearrangements, and that this drug combination may be used to target a network of changes in cancer.
"The results also demonstrate the benefits of using a combined screening, proteomics and computer-based modeling approach to identify drugs that act on multiple targets and to determine how they function," said study lead author Uwe Rix, Ph.D., assistant member of the Drug Discovery Program at Moffitt.
"In the future, this strategy may facilitate further drug repurposing efforts and lead to an increase in new therapy options for patients with difficult-to-treat diseases."
Source-Eurekalert