DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs or DNA Hypomethylating Agents in MLL-Rearranged.

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DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs or DNA Hypomethylating Agents in MLL-Rearranged Leukemia Cells by Christine R Klaus, Scott R. Daigle, Dorothy Iwanowics, L. Danielle Johnston, Carly A Therkelsen, Jesse J Smith, Mikel P Moyer, Robert A. Copeland, Edward J Olhava, Margaret Porter Scott, Roy M. Pollock, and Alejandra Raimondi Blood Volume 122(21):3930-3930 November 15, 2013 ©2013 by American Society of Hematology

Figure 1. Fa-CI plots show that EPZ-5676 and cytarabine act synergistically to induce an antiproliferative effect in the Molm-13 cell line in a pre-treatment model. Figure 1. Fa-CI plots show that EPZ-5676 and cytarabine act synergistically to induce an antiproliferative effect in the Molm-13 cell line in a pre-treatment model. (A) Ten-day continuous dosing of EPZ-5676 with addition of cytarabine at day 7 showed a range of fractional effects with CI values <1 denoting synergy. (B) EPZ-5676 was removed at day 7 prior to the addition of cytarabine showing durable combination benefit. Scott R. Daigle et al. Blood 2013;122:3930 ©2013 by American Society of Hematology