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Constellation has two clinical-stage oncology development programs.

The first 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. The first clinical trials of CPI-0610 are being conducted in patients with lymphoma, leukemia, and myeloma.

The second program is evaluating a compound called CPI-1205, a small molecule that inhibits an enzyme called Enhancer of Zeste Homolog 2 (EZH2). EZH2 is part of a complex of several proteins, called the PRC2 complex, which is involved in the regulation of gene expression. The PRC2 complex generally suppresses (“turns off”) the expression of the genes with which it is associated. EZH2 contributes to this suppression of gene expression by facilitating a reaction in which a small chemical group, called a methyl group (- CH3), is added to one of the proteins (called a histone protein) that is normally associated with genes (DNA). By inhibiting (blocking) the activity of EZH2, CPI-1205 may allow cancer-suppressing genes to be turned back on and thereby have an anti-cancer effect. The first clinical trial of CPI-1205 is being conducted in patients with lymphoma.

Constellation is currently conducting the following studies:

CPI-0610 and CPI-1205 are investigational drugs, meaning they not been approved by the FDA (or any other regulatory authority) and, as such, are not available for use outside of a clinical trial setting.