The Leukemia and Lymphoma Society is providing Constellation Pharmaceuticals with up to $7.5 million to support the continued preclinical and early clinical development of small molecule BET inhibitor drugs for the treatment of hematologic cancers. The firm says inhibition of the bromodomain and extra-terminal—or BET—family of chromatin adaptors modulates gene expression and leads to the death of tumor cells across a range of hematologic malignancies and some solid tumors.

Constellation is exploiting expertise in the field of abnormal epigenetic regulation of gene expression, to build a pipeline of small molecule therapeutics for the treatment of cancer, inflammatory/immunologic disorders, and other diseases. The firm’s drug discovery product engine, including screening strategies and structure-based drug design, has already yielded potent and selective inhibitors of BET bromodomains. Last year Constellation published preclinical data demonstrating that small molecule BET protein bromodomain inhibitors suppress the transcription of MYC, which plays a role in a number of cancers. Additional emerging data also indicate that small molecule BET inhibition blocks the expression of NF-kB-dependent genes and BCL-2, which are also implicated in cancer and inflammation.

The Constellation partnership has been established through LLS’s Therapy Acceleration Program, through which the organization partners directly with biotech firms to help speed the identification and development of promising drugs. “We are very pleased to be partnering with Constellation on the further development of its leading BET inhibitor program so that we can more quickly determine how this new class of drugs can have the greatest impact for patients with these diseases.” 

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