Constellation has two clinical-stage oncology development programs:
CPI-0610 is a small molecule that inhibits the expression of several genes involved in cancer. One of the genes targeted by CPI-0610 is called MYC, which is frequently overexpressed (“turned on”) in both blood cancers and some solid tumors. CPI-0610 suppresses the expression of MYC and other cancer-related genes by interfering with the binding of a family of proteins, known as BET proteins, to these genes. Clinical trials of CPI-0610 are currently being conducted in patients with lymphoma, leukemia and multiple myeloma.
CPI-1205 is a small molecule that increases the expression of genes that are abnormally suppressed (“turned off”) in some cancers. CPI-1205 blocks the activity of an enzyme called EZH2. EZH2 normally places a small chemical group, called a methyl group, on a protein associated with DNA. When the methyl group is placed on the protein the gene in this location is less likely to be expressed. While this effect of EZH2 on gene expression is a normal part of development, some cancers depend on an abnormal pattern of gene expression caused by EZH2. The first clinical trial of CPI-1205 is being conducted in patients with lymphoma.
Constellation is currently conducting the following studies:
- A Phase 1 clinical study of CPI-0610 in patients with lymphoma. For more information about this study, click here.
- A Phase 1 clinical study of CPI-0610 in patients with acute leukemia, myelodysplastic syndrome, myelodysplastic/myeloproliferative neoplasms or myelofibrosis. For more information about this study, click here.
- A Phase 1 clinical study of CPI-0610 in patients with multiple myeloma. For more information about this study, click here.
- A Phase 1 clinical study of CPI-1205 in patients with lymphoma. For more information about this study, click here.
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.
The Leukemia & Lymphoma Society (LLS) has been a partner with Constellation Pharmaceuticals since 2013. LLS has provided funding for all three of the ongoing studies of CPI-0610, Constellation’s lead BET inhibitor, in patients with lymphoma, leukemia and myeloma. LLS helps patients with these diseases in many other ways, including personalized searches for relevant clinical trials and support services. For more information about LLS, go to: www.lls.org.