On May 20, 2019 Constellation Pharmaceuticals, Inc. (Nasdaq: CNST) reported that Dr. Patricia Keller, Senior Scientist at Constellation Pharmaceuticals, presented a poster titled Targeting epigenetic dysregulation in bladder cancer through inhibition of EZH2 at the Bladder Cancer: Transforming the Field meeting of the American Association for Cancer Research (AACR) (Free AACR Whitepaper) in Denver on May 19 (Press release, Constellation Pharmaceuticals, MAY 20, 2019, View Source [SID1234536473]).

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The poster discusses results of Constellation’s work with its second-generation EZH2 inhibitor CPI-0209 in bladder cancer models, exploring whether ARID1A mutation status affected responsiveness to CPI-0209 treatment. ARID1A, a protein that is a key component of the SWI/SNF chromatin remodeling complex, is mutated in about 25% of muscle-invasive bladder cancers.

Constellation used CPI-0209 in long-term phenotypic growth assays in a panel of 21 bladder cancer cell lines, demonstrating preferential treatment sensitivity that correlated with increased cell death in cell lines harboring ARID1A mutations. Transcriptional profiling after CPI-0209 treatment showed widespread activation of EZH2 target gene expression. In vivo, once-daily treatment with CPI-0209 in bladder cell-line derived xenografts harboring ARID1A mutations produced dose-dependent tumor growth inhibition and regression. Treatment with CPI-0209 and the chemotherapeutic agent cisplatin demonstrated combinatorial effects on cell viability in vitro and on tumor growth in vivo. The poster can be viewed in the Investors & Media/Presentations section of our website.