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Constellation’s first oncology clinical program is evaluating a compound called CPI-0610, a small molecule that inhibits the binding of bromodomain and extra terminal (BET) proteins to chromatin. Chromatin is the combination of DNA, the building block of all genes, and its associated proteins.   BET proteins enable the expression ("switching on") of a limited number of genes, some of which are implicated in causing cancer.  For example, the cancer gene known as MYC often depends on BET proteins in order to be expressed. When CPI-0610 binds to BET proteins it causes the expression of MYC to decrease. This effect of CPI-0610 on the expression of MYC and other cancer genes is thought to be the reason why it may be effective in treating cancer.

Constellation is currently conducting the following study:

CPI-0610 is an investigational drug, meaning it has not been approved by the FDA (or any other regulatory authority) and, as such, is not available for use outside of a clinical trial setting.