V158411
Summary
Some cancer cells use the Chk1 pathway to increase cell survival by pausing DNA replication and allowing repair of the damaged DNA before completing cell division. Inhibition of Chk1 blocks this pathway, forcing cells to undergo cell division (mitosis) with substantial DNA damage that results in their death.
The aim of our research programme was to identify product candidates that increase the anti-tumour efficacy of current cytotoxic agents without increasing their toxicity to non-cancerous tissues. V158411 met these goals in pre-clinical cancer models when administered with commonly used cytotoxic agents, and has drug-like characteristics and appropriate pharmacokinetic properties.
Because Chk1 inhibitors are used in conjunction with chemotherapy drugs, they can potentially be used to treat a broad range of tumour types including breast, prostate, colorectal and melanoma. They may also be used in haematological cancers such as leukaemia.
