42O - A Phase 1 Study of CPI-1205, a Small Molecule Inhibitor of EZH2, Preliminary Safety in Patients with B-Cell Lymphomas

Date 06 March 2018
Event TAT 2018 - Targeted Anticancer Therapies
Session Proffered Paper Session 2
Topics Anti-Cancer Agents & Biologic Therapy
Haematologic Malignancies
Presenter Adrian Senderowicz
Citation Annals of Oncology (2018) 29 (suppl_3): iii7-iii9. 10.1093/annonc/mdy048
Authors W. Harb1, J. Abramson2, M. Lunning3, A. Goy4, K. Maddocks5, C. Lebedinsky6, A. Senderowicz7, P. Trojer7, W.D. Bradley7, I. Flinn8
  • 1Horizon Oncology Center, 47905 - Lafayette/US
  • 2Massachusetts General Hospital Cancer Center, Boston/US
  • 3University of Nebraska Medical Center, Omaha/US
  • 4Hackensack University Medical Center, Hackensack/US
  • 5Ohio State University Comprehensive Cancer Center, Columbus/US
  • 6Constellation Pharmaceuticals, 02142 - Cambridge/US
  • 7Constellation Pharmaceuticals, Cambridge/US
  • 8Sarah Cannon Research Institute, Nashville/US


EZH2 is the catalytic subunit of the PRC2 complex, and plays an important role in transcriptional repression. EZH2 over-expression is correlated with poor prognosis. Hot spot mutations in EZH2 were first identified in GCB-DLBCL and follicular lymphoma (FL). CPI-1205 is a potent, selective, SAM-competitive EZH2 inhibitor. A Phase I study was conducted in B-cell lymphoma patients. Primary Objectives: Define maximum tolerated dose of CPI-1205 and the dose-limiting toxicities (DLTs).