Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

Filippakopoulos, 2014, Targeting bromodomains: epigenetic readers of lysine acetylation, Nat Rev Drug Discov, 13, 337, 10.1038/nrd4286

Lovén, 2013, Selective inhibition of tumor oncogenes by disruption of super-enhancers, Cell, 153, 320, 10.1016/j.cell.2013.03.036

Chapuy, 2013, Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma, Cancer Cell, 24, 777, 10.1016/j.ccr.2013.11.003

Filippakopoulos, 2010, Selective inhibition of BET bromodomains, Nature, 468, 1067, 10.1038/nature09504

Noel, 2013, Development of the BET bromodomain inhibitor OTX015, Mol Cancer Ther, 12, C244, 10.1158/1535-7163.TARG-13-C244

Boi, 2015, The BET bromodomain inhibitor OTX015 affects pathogenetic pathways in preclinical B-cell tumor models and synergizes with targeted drugs, Clin Cancer Res, 21, 1628, 10.1158/1078-0432.CCR-14-1561

Trabucco, 2015, Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma, Clin Cancer Res, 21, 113, 10.1158/1078-0432.CCR-13-3346

Delmore, 2011, BET bromodomain inhibition as a therapeutic strategy to target c-Myc, Cell, 146, 904, 10.1016/j.cell.2011.08.017

Chesi, 2012, Drug response in a genetically engineered mouse model of multiple myeloma is predictive of clinical efficacy, Blood, 120, 376, 10.1182/blood-2012-02-412783

Berthon, 2016, Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study, Lancet Haematol, 10.1016/S2352-3026(15)00247-1

Cheson, 2007, Revised response criteria for malignant lymphoma, J Clin Oncol, 25, 579, 10.1200/JCO.2006.09.2403

Odore, 2014, Development and validation of an UPLC-MS/MS method for quantitative analysis of OTX015 in human plasma samples, Anal Methods, 6, 9108, 10.1039/C4AY02249A

Odore, 2015, Phase I population pharmacokinetic assessment of the oral bromodomain inhibitor OTX015 in patients with haematologic malignancies, Clin Pharmacokinet

Cheson, 2007, Revised response criteria for malignant lymphoma, J Clin Oncol, 25, 579, 10.1200/JCO.2006.09.2403

Durie, 2006, International uniform response criteria for multiple myeloma, Leukemia, 20, 1467, 10.1038/sj.leu.2404284

Hans, 2004, Confirmation of the molecular classification of diffuse large B-cell lymphoma by immunohistochemistry using a tissue microarray, Blood, 103, 275, 10.1182/blood-2003-05-1545

Pfreundschuh, 2012, Growing importance of MYC/BCL2 immunohistochemistry in diffuse large B-cell lymphomas, J Clin Oncol, 30, 3433, 10.1200/JCO.2012.44.4729

Mottamal, 2015, Histone deacetylase inhibitors in clinical studies as templates for new anticancer agents, Molecules, 20, 3898, 10.3390/molecules20033898

Coudé, 2015, BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells, Oncotarget, 6, 17698, 10.18632/oncotarget.4131

Whitfield, 2012, Tumor microenvironment: becoming sick of Myc, Cell Mol Life Sci, 69, 931, 10.1007/s00018-011-0860-x

Dang, 2012, MYC on the path to cancer, Cell, 149, 22, 10.1016/j.cell.2012.03.003

Petrich, 2014, MYC-associated and double-hit lymphomas: a review of pathobiology, prognosis, and therapeutic approaches, Cancer, 120, 3884, 10.1002/cncr.28899

Perry, 2014, MYC and BCL2 protein expression predicts survival in patients with diffuse large B-cell lymphoma treated with rituximab, Br J Haematol, 165, 382, 10.1111/bjh.12763

Thieblemont, 2013, MYC, BCL2, BCL6 in DLBCL: impact for clinics in the future?, Blood, 121, 2165, 10.1182/blood-2013-01-480392

Bhadury, 2014, BET bromodomain inhibitors abrogate cell cycle progression and induces apoptosis in Myc-induced mouse lymphoma cells without affecting MYC transcription. Abstract 5495, Cancer Res, 74, 5495, 10.1158/1538-7445.AM2014-5495

Bhadury, 2014, BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma, Proc Natl Acad Sci USA, 111, E2721, 10.1073/pnas.1406722111