Benzinga | Jun 4, 2021 09:22AM EDT

Constellation Pharmaceuticals Presents Phase 1 Data for CPI-0209 at ASCO Annual Meeting

Constellation Pharmaceuticals, Inc. (NASDAQ:CNST), a clinical-stage biopharmaceutical company using its expertise in epigenetics to discover and develop novel therapeutics, today summarized in a poster presentation preliminary data from the ongoing Phase 1/2 trial of CPI-0209, a novel, second-generation, small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2). These data were published online in conjunction with the American Society of Clinical Oncology (ASCO) Annual Meeting, and show comprehensive target engagement and durable exposure of CPI-0209. Anti-tumor activity of CPI-0209 in pre-clinical models was demonstrated across several advanced hematologic and solid tumor types.

"We designed CPI-0209 to improve on first-generation EZH2 inhibitors in a number of ways, including increased potency, long residence time on target, and a lack of auto-induction of metabolism. These enhancements translate in the clinic, which we believe will be key to unlocking the full therapeutic potential of EZH2 inhibition," said Jigar Raythatha, president and chief executive officer of Constellation Pharmaceuticals. "I am also pleased that dosing is under way in our Phase 2 expansion cohorts at the selected dose."