The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

Authors: Eytan M. Stein, Guillermo Garcia‐Manero, David A. Rizzieri, Raoul Tibes, Jesús G. Berdeja, Michael R. Savona, Mojca Jongen-Lavrenic, Jessica K. Altman, Blythe Thomson, Stephen J. Blakemore, Scott R. Daigle, Nigel J. Waters, A. Benjamin Suttle, Alicia Clawson, Roy M. Pollock, Andrei V. Krivtsov, Scott A. Armstrong, Jorge DiMartino, Eric Hedrick, Bob Löwenberg, Martin S. Tallman - Blood 2018 cited by 457

Key Points Pinometostat demonstrates first evidence of DOT1L target inhibition and clinical responses in a subset of MLL-r advanced leukemia patients. The observed safety profile of pinometostat shows potential for exploration of combination therapies in leukemia.