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Constellation Pharmaceuticals is a clinical-stage biopharmaceutical company using its expertise in epigenetics to discover and develop novel therapeutics that address serious unmet medical needs in patients with cancers associated with abnormal gene expression or drug resistance. The company’s integrated epigenetics platform enables it to validate targets and generate small molecules against these targets that selectively modulate gene expression in tumor and immune cells to drive anti-tumor activity.

Platform insights and clinical experience guide development of Constellation Pharmaceuticals’ wholly owned lead product candidates: CPI-1205, which inhibits enhancer of zeste homolog 2, or EZH2, and CPI-0610, which inhibits bromodomain and extra terminal domain, or BET, proteins. The company believes that its approach to targeting these central gene regulatory mechanisms associated with cancer proliferation may enable it to provide therapeutic benefits to cancer patients.

Constellation’s integrated epigenetics platform includes a deep understanding of the biology of regulation of gene expression by epigenetic regulatory proteins, or epigenetic regulators, the development of small-molecule product candidates that selectively modulate their activity and the design of clinical development programs supported by novel biomarker strategies. The company is able to target a broad variety of epigenetic regulators using its platform and has generated development candidates acting against distinct classes of those regulators. It utilized its epigenetics platform to discover and design CPI-1205, CPI-0610 and CPI-0209, which is a second-generation EZH2 inhibitor, and continues to leverage this platform to develop these product candidates and to discover and develop additional product candidates.

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