A novel drug may be effective against haematological malignancies and is already being tested in early clinical trials, it has been announced.
Fadraciclib inhibits two cancer-driving proteins in the cyclin-dependent kinase family, CDK2 and CDK9. It is based on an earlier CDK inhibitor called seliciclib. Improvements to its chemical properties now mean that fadraciclib is 20 times more potent against the CDK2 and CDK9 targets. This translates to a 30-fold increase in therapeutic potency against human cancer cells, say the researchers.
The drug has been jointly developed by researchers at the Institute of Cancer Research in London in collaboration with the company Cyclacel, based in Dundee. Details appeared recently in the journal PLoS One.
The authors write: “Over the last two decades substantial efforts have been directed towards identification and development of pharmaceutical CDK inhibitors.
“Fadraciclib exhibits improved potency and selectivity for CDK2 and CDK9 compared to seliciclib, and also displays high selectivity.
“This cellular potency and mechanism of action translate to promising anti-cancer activity in human leukaemia mouse xenograft models.”
The team also found that combining fadraciclib with BCL2 inhibitors has a synergistic effect against leukaemia cell lines.
They conclude that these findings “support its therapeutic potential in CDK9- or CDK2-dependent cancers and as a rational combination with BCL2 inhibitors in haematological malignancies.”
Researcher Professor Paul Workman, says: “These new results […] detail research that has already led to clinical trials of fadraciclib in various cancer types, and we hope will result in new targeted treatments for patients with leukaemias and solid cancers.”
Frame S, Saladino C, MacKay C, Atrash B, Sheldrake P, McDonald E, Clarke PA, Workman P, Blake D, Zheleva D (2020) “Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer.” PLoS One, doi: 10.1371/journal.pone.0234103
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