| 2015 | A Medium-Throughput Single Cell CRISPR/Cas9 Assay to Assess Gene Essentiality | EZH2 | National Center for Biotechnology Information | A Medium-Throughput Single Cell CRISPR/Cas9 Assay to Assess Gene Essentiality |
| 2017 | Activity of EZH2 inhibitors as monotherapy and in combination with multiple myeloma therapies | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | Activity of EZH2 inhibitors as monotherapy and in combination with multiple myeloma therapies |
| 2017 | ASH 2017 G9a Poster | EHMT 1/2 | American Society of Hematology (ASH) | ASH 2017 G9a Poster |
| 2019 | CRPC Preclinical Data Presentation AACR-NCI-EORTC 2019 | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | CRPC Preclinical Data Presentation AACR-NCI-EORTC 2019 |
| 2013 | EZH2 Inhibitor EPZ-6438 Synergizes With Anti-Lymphoma Therapies in Preclinical Models | EZH2 (tazemetostat) | American Society of Hematology (ASH) | EZH2 Inhibitor EPZ-6438 Synergizes With Anti-Lymphoma Therapies in Preclinical Models |
| 2014 | Small Molecule Control of Chromatin Remodeling | EZH2 | Chemistry & Biology Review | Small Molecule Control of Chromatin Remodeling |
| 2020 | A Phase 1b/2 Open-Label Study Evaluating Tazemetostat in Combination with Enzalutamide or Abiraterone/Prednisone in Chemotherapy-Naive Patients With Metastatic Castration-Resistant Prostate Cancer | EZH2 (tazemetostat) | American Society of Clinical Oncology – Genitourinary Cancers Symposium (ASCO-GU) | A Phase 1b/2 Open-Label Study Evaluating Tazemetostat in Combination with Enzalutamide or Abiraterone/Prednisone in Chemotherapy-Naive Patients With Metastatic Castration-Resistant Prostate Cancer |
| 2020 | A Phase 1b/3 Global Randomized, Double-blind, Placebo-controlled Study of Tazemetostat in Combination with Doxorubicin as Frontline Therapy for Advanced Epithelioid Sarcoma | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | A Phase 1b/3 Global Randomized, Double-blind, Placebo-controlled Study of Tazemetostat in Combination with Doxorubicin as Frontline Therapy for Advanced Epithelioid Sarcoma |
| 2020 | A Phase 1b/3 Randomized, Double-Blind, 3-Stage Study of Tazemetostat or Placebo Plus Lenalidomide and Rituximab in Patients With Relapsed/Refractory Follicular Lymphoma | EZH2 (tazemetostat) | American Society of Hematology (ASH) | A Phase 1b/3 Randomized, Double-Blind, 3-Stage Study of Tazemetostat or Placebo Plus Lenalidomide and Rituximab in Patients With Relapsed/Refractory Follicular Lymphoma |
| 2018 | A Phase 2, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults (Epithelioid Sarcoma Cohort) (NCT02601950) | EZH2 (tazemetostat) | European Society for Medical Oncology (ESMO) | A Phase 2, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults (Epithelioid Sarcoma Cohort) (NCT02601950) |
| 2018 | A Phase 2, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults (INI1-Negative Tumors Cohort) (NCT02601950) | EZH2 (tazemetostat) | European Society for Medical Oncology (ESMO) | A Phase 2, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults (INI1-Negative Tumors Cohort) (NCT02601950) |
| 2018 | A Phase 2, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults (Rhabdoid Tumor Cohort) (NCT02601950) | EZH2 (tazemetostat) | European Society for Medical Oncology (ESMO) | A Phase 2, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults (Rhabdoid Tumor Cohort) (NCT02601950) |
| 2020 | Aberrant SWI/SNF complexes lacking SMARCA2 or SMARCA4 differentially affect cell state and response to a novel SMARCA2/4 inhibitor | SMARCA2/4 | American Association for Cancer Research (AACR) | Aberrant SWI/SNF complexes lacking SMARCA2 or SMARCA4 differentially affect cell state and response to a novel SMARCA2/4 inhibitor |
| 2020 | Analyzing Efficacy Outcomes From the Phase 2 Study of Single-Agent Tazemetostat as Third-Line Therapy in Patients With Relapsed or Refractory Follicular Lymphoma to Identify Predictors of Response | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Analyzing Efficacy Outcomes From the Phase 2 Study of Single-Agent Tazemetostat as Third-Line Therapy in Patients With Relapsed or Refractory Follicular Lymphoma to Identify Predictors of Response |
| 2021 | Budget Impact Analysis of Tazemetostat for Third-Line or Later (3L+) Relapsed or Refractory Follicular Lymphoma | EZH2 (tazemetostat) | Academy of Managed Care Pharmacy (AMCP) 2021 | Budget Impact Analysis of Tazemetostat for Third-Line or Later (3L+) Relapsed or Refractory Follicular Lymphoma |
| 2017 | Discovery of Candidate Predictors of Response to Tazemetostat in Diffuse Large B-Cell Lymphoma and Follicular Lymphoma using NGS Technology on ctDNA Samples Collected Pre-treatment | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Discovery of Candidate Predictors of Response to Tazemetostat in Diffuse Large B-Cell Lymphoma and Follicular Lymphoma using NGS Technology on ctDNA Samples Collected Pre-treatment |
| 2019 | Drug-Drug Interaction Potential of EZH2 Inhibitor Tazemetostat | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | Drug-Drug Interaction Potential of EZH2 Inhibitor Tazemetostat |
| 2020 | Efficacy and Safety of Tazemetostat in Patients With INI1/SMARCB1- or BRG1/SMARCA4-Negative Tumors, or Relapsed/Refractory Synovial Sarcoma | EZH2 (tazemetostat) | Connective Tissue Oncology Society (CTOS) | Efficacy and Safety of Tazemetostat in Patients With INI1/SMARCB1- or BRG1/SMARCA4-Negative Tumors, or Relapsed/Refractory Synovial Sarcoma |
| 2020 | Efficacy, Safety, and Immune Priming Effect of Tazemetostat in Patients With Epithelioid Sarcoma | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | Efficacy, Safety, and Immune Priming Effect of Tazemetostat in Patients With Epithelioid Sarcoma |
| 2020 | EZH2 Gain-of-Function Mutations Are Not Associated With More Favorable Prognosis in Relapsed/Refractory Follicular Lymphoma: A Preliminary Analysis on 908 Patients | EZH2 (tazemetostat) | European School of Hematology (ESH) | EZH2 Gain-of-Function Mutations Are Not Associated With More Favorable Prognosis in Relapsed/Refractory Follicular Lymphoma: A Preliminary Analysis on 908 Patients |
| 2021 | EZH2 Inhibitor Tazemetostat Demonstrates Activity in Preclinical Models of Bruton’s Tyrosine Kinase Inhibitor-Resistant Relapsed/Refractory Mantle Cell Lymphoma | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | EZH2 Inhibitor Tazemetostat Demonstrates Activity in Preclinical Models of Bruton’s Tyrosine Kinase Inhibitor-Resistant Relapsed/Refractory Mantle Cell Lymphoma |
| 2018 | High Concordance Observed Between Local and Central INI1 Immunohistochemistry Results Obtained From Clinical Studies EZH-102 and EZH-202 | EZH2 (tazemetostat) | American Society of Clinical Pathology (ASCP) | High Concordance Observed Between Local and Central INI1 Immunohistochemistry Results Obtained From Clinical Studies EZH-102 and EZH-202 |
| 2020 | Identification of a potent, orally-available SMARCA2 inhibitor with in vitro and in vivo activity in preclinical models of SMARCA4-mutant NSCLC | SMARCA4 | American Association for Cancer Research (AACR) | Identification of a potent, orally-available SMARCA2 inhibitor with in vitro and in vivo activity in preclinical models of SMARCA4-mutant NSCLC |
| 2020 | Integrated Safety Analysis of Tazemetostat 800 mg Twice Daily in Adult Patients with Hematologic and Solid Tumors | EZH2 (tazemetostat) | European Society for Medical Oncology (ESMO) | Integrated Safety Analysis of Tazemetostat 800 mg Twice Daily in Adult Patients with Hematologic and Solid Tumors |
| 2018 | Interim Results from an Ongoing Phase 2 Multicenter Study of Tazemetostat, an EZH2 Inhibitor, in Patients with Relapsed or Refractory (R/R) Diffuse Large B-cell Lymphoma (DLBCL) | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Interim Results from an Ongoing Phase 2 Multicenter Study of Tazemetostat, an EZH2 Inhibitor, in Patients with Relapsed or Refractory (R/R) Diffuse Large B-cell Lymphoma (DLBCL) |
| 2021 | Kinetics of Response to Tazemetostat in Patients With Relapsed or Refractory Follicular Lymphoma | EZH2 (tazemetostat) | Annual International Congress on Hematologic Malignancies: Focus on Leukemias, Lymphomas, and Myeloma | Kinetics of Response to Tazemetostat in Patients With Relapsed or Refractory Follicular Lymphoma |
| 2018 | Molecular characterization of epithelioid sarcoma (ES) tumors derived from patients enrolled in a phase 2 study of tazemetostat (NCT02601950) | EZH2 (tazemetostat) | European Society for Medical Oncology (ESMO) | Molecular characterization of epithelioid sarcoma (ES) tumors derived from patients enrolled in a phase 2 study of tazemetostat (NCT02601950) |
| 2020 | Phase 1 Multicenter Study to Characterize the Pharmacokinetics of intravenous (IV) and Orally Administered, [14C]-Labeled Tazemetostat in Patients With B-Cell Lymphomas or Advanced Solid Tumors | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | Phase 1 Multicenter Study to Characterize the Pharmacokinetics of intravenous (IV) and Orally Administered, [14C]-Labeled Tazemetostat in Patients With B-Cell Lymphomas or Advanced Solid Tumors |
| 2020 | Phase 1 Study of Tazemetostat, an Enhancer of Zeste Homolog-2 Inhibitor in Pediatric Patients With Relapsed/Refractory Integrase Interactor 1-Negative Tumors | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | Phase 1 Study of Tazemetostat, an Enhancer of Zeste Homolog-2 Inhibitor in Pediatric Patients With Relapsed/Refractory Integrase Interactor 1-Negative Tumors |
| 2017 | Phase 1 Study of the EZH2 Inhibitor, Tazemetostat, in Children With Relapsed or Refractory INI1-Negative Tumors Including Rhabdoid Tumors, Epithelioid Sarcoma, Chordoma; and Synovial Sarcoma | EZH2 (tazemetostat) | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | Phase 1 Study of the EZH2 Inhibitor, Tazemetostat, in Children With Relapsed or Refractory INI1-Negative Tumors Including Rhabdoid Tumors, Epithelioid Sarcoma, Chordoma; and Synovial Sarcoma |
| 2018 | Phase 2 Multicenter Study of the EZH2 Inhibitor Tazemetostat as Monotherapy in Adults With Relapsed or Refractory Malignant Mesothelioma With BAP1 Inactivation | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | Phase 2 Multicenter Study of the EZH2 Inhibitor Tazemetostat as Monotherapy in Adults With Relapsed or Refractory Malignant Mesothelioma With BAP1 Inactivation |
| 2017 | Phase 2 Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults With Synovial Sarcoma | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | Phase 2 Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adults With Synovial Sarcoma |
| 2017 | Preliminary evidence of a molecular predictor of tazemetostat response, beyond EZH2 mutation, in NHL patients via characterization of archive tumor and circulating tumor DNA | EZH2 (tazemetostat) | International Conference on Malignant Lymphoma (ICML) | Preliminary evidence of a molecular predictor of tazemetostat response, beyond EZH2 mutation, in NHL patients via characterization of archive tumor and circulating tumor DNA |
| 2017 | Response to the EZH2 Inhibitor Tazemetostat Is Independent of Cell of Origin Determined Via Hans Immunohistochemistry or NanoString Lymphoma Subtyping Test in EZH2 Wild-Type DLBCL Patients | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Response to the EZH2 Inhibitor Tazemetostat Is Independent of Cell of Origin Determined Via Hans Immunohistochemistry or NanoString Lymphoma Subtyping Test in EZH2 Wild-Type DLBCL Patients |
| 2020 | Safety and Efficacy of Tazemetostat, an Enhancer of Zeste Homolog 2 Inhibitor, in Patients With Relapsed or Refractory Malignant Mesothelioma | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | Safety and Efficacy of Tazemetostat, an Enhancer of Zeste Homolog 2 Inhibitor, in Patients With Relapsed or Refractory Malignant Mesothelioma |
| 2019 | Synergistic activity of tazemetostat in combination with androgen signaling inhibitors in preclinical models of prostate cancer demonstrates potential for clinical expansion | EZH2 (tazemetostat) | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | Synergistic activity of tazemetostat in combination with androgen signaling inhibitors in preclinical models of prostate cancer demonstrates potential for clinical expansion |
| 2020 | Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial (for HCPs only) | EZH2 (tazemetostat) | Lancet Oncology | Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial (for HCPs only) |
| 2020 | Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study (for HCPs only) | EZH2 (tazemetostat) | Lancet Oncology | Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study (for HCPs only) |
| 2020 | Tazemetostat Is Associated With Lower Risk for Safety Outcomes Versus the PI3-Kinases Idelalisib, Duvelisib and Copanlisib, in Patients With Relapsed/Refractory Follicular Lymphoma Who Have Received at Least 2 Prior Systemic Treatments: a Matching-Adjusted Indirect Comparison of Single-Arm Trials | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Tazemetostat Is Associated With Lower Risk for Safety Outcomes Versus the PI3-Kinases Idelalisib, Duvelisib and Copanlisib, in Patients With Relapsed/Refractory Follicular Lymphoma Who Have Received at Least 2 Prior Systemic Treatments: a Matching-Adjusted Indirect Comparison of Single-Arm Trials |
| 2020 | Trial in Progress: A Phase 2, Open-Label, Multicenter Study of Tazemetostat in Combination With Rituximab for the Treatment of Relapsed or Refractory Follicular Lymphoma | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Trial in Progress: A Phase 2, Open-Label, Multicenter Study of Tazemetostat in Combination With Rituximab for the Treatment of Relapsed or Refractory Follicular Lymphoma |
| 2018 | Updated Report on Identification of Molecular Predictors of Tazemetostat Response in an Ongoing NHL Phase 2 Study | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Updated Report on Identification of Molecular Predictors of Tazemetostat Response in an Ongoing NHL Phase 2 Study |
| 2015 | A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening | General | Journal of Biomolecular Screening | A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening |
| 2015 | A Medium-Throughput Single Cell CRISPR-Cas9 Assay to Assess Gene Essentiality | EZH2 | Biological Procedures Online | A Medium-Throughput Single Cell CRISPR-Cas9 Assay to Assess Gene Essentiality |
| 2012 | A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells | EZH2 | Nature Chemical Biology | A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells |
| 2015 | A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models | PRMT5 | Nature Chemical Biology | A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models |
| 2012 | A687V EZH2 is a gain-of-function mutation found in lymphoma patients | EZH2 | FEBS Letters | A687V EZH2 is a gain-of-function mutation found in lymphoma patients |
| 2018 | Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing | PRMT5 | Scientific Reports | Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing |
| 2019 | Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss | PRMT5 | Cancer Cell | Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss |
| 2015 | Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound | PRMT6 | ACS Medicinal Chemistry Letters | Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound |
| 2018 | ASCO 2018 Mesothelioma Poster | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | ASCO 2018 Mesothelioma Poster |
| 2016 | CARM1 Preferentially Methylates H3R17 over H3R26 through a Random Kinetic Mechanism | CARM1 | Biochemistry | CARM1 Preferentially Methylates H3R17 over H3R26 through a Random Kinetic Mechanism |
| 2016 | Characterization of Inhibitor Binding Through Multiple Inhibitor Analysis: A Novel Local Fitting Method | General | Methods in Molecular Biology | Characterization of Inhibitor Binding Through Multiple Inhibitor Analysis: A Novel Local Fitting Method |
| 2016 | Characterization of the Enzymatic Activity of SETDB1 and Its 1:1 Complex with ATF7IP | SETDB1 | Biochemistry | Characterization of the Enzymatic Activity of SETDB1 and Its 1:1 Complex with ATF7IP |
| 2011 | Chemogenetic analysis of human protein methyltransferases | General | Chemical Biology & Drug Design | Chemogenetic analysis of human protein methyltransferases |
| 2017 | Chemosensitive Relapse in Small Cell Lung Cancer Proceeds through an EZH2-SLFN11 Axis | EZH2 | Cancer Cell | Chemosensitive Relapse in Small Cell Lung Cancer Proceeds through an EZH2-SLFN11 Axis |
| 2012 | Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L | DOT1L | Chemical Biology & Drug Design | Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L |
| 2011 | Conformational adaptation in drug-target interactions and residence time | General | Future Medicinal Chemistry | Conformational adaptation in drug-target interactions and residence time |
| 2013 | Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys²⁷ methylation by human polycomb repressive complex 2 and vSET | EZH2 | Biochemical Journal | Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys²⁷ methylation by human polycomb repressive complex 2 and vSET |
| 2010 | Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas | EZH2 | Proceedings of the National Academy of Sciences of the United States of America (PNAS) | Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas |
| 2015 | CRISPR Pooled Screening Identifies Differential Dependencies on Epigenetic Pathways | EZH2 | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | CRISPR Pooled Screening Identifies Differential Dependencies on Epigenetic Pathways |
| 2016 | DOT1L as a therapeutic target for the treatment of DNMT3A-mutant acute myeloid leukemia | EZH2 | Blood | DOT1L as a therapeutic target for the treatment of DNMT3A-mutant acute myeloid leukemia |
| 2014 | DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells | DOT1L | Journal of Pharmacology and Experimental Therapeutics | DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells |
| 2017 | Drug Discovery and Chemical Biology of Cancer Epigenetics | General | Cell Chemical Biology | Drug Discovery and Chemical Biology of Cancer Epigenetics |
| 2013 | Drugging the human methylome: an emerging modality for reversible control of aberrant gene transcription | General | Current Opinion in Chemical Biology | Drugging the human methylome: an emerging modality for reversible control of aberrant gene transcription |
| 2016 | Drug-target interaction kinetics: underutilized in drug optimization? | DOT1L | Future Medicinal Chemistry | Drug-target interaction kinetics: underutilized in drug optimization? |
| 2015 | Drug-target interactions: Stay tuned | General | Nature Chemical Biology | Drug-target interactions: Stay tuned |
| 2011 | Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 | EZH2 | Proceedings of the National Academy of Sciences of the United States of America (PNAS) | Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 |
| 2015 | Epigenetic Medicinal Chemistry | General | ACS Medicinal Chemistry Letters | Epigenetic Medicinal Chemistry |
| 2013 | Epizyme® announces that the “Nature Reprint Collection: Epigenetics” from Nature Publishing Group is now available online | General | Nature Reprint Collection | Epizyme® announces that the “Nature Reprint Collection: Epigenetics” from Nature Publishing Group is now available online |
| 2015 | EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity | EZH2 | ACS Medicinal Chemistry Letters | EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity |
| 2019 | Establishing and Maintaining a Robust Sample Management System | General | SLAS Technology | Establishing and Maintaining a Robust Sample Management System |
| 2015 | Exploring drug delivery for the DOT1L inhibitor pinometostat (EPZ-5676): Subcutaneous administration as an alternative to continuous IV infusion, in the pursuit of an epigenetic target | DOT1L | Journal of Controlled Release | Exploring drug delivery for the DOT1L inhibitor pinometostat (EPZ-5676): Subcutaneous administration as an alternative to continuous IV infusion, in the pursuit of an epigenetic target |
| 2017 | EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL | EZH2 (tazemetostat) | Molecular Cancer Therapeutics | EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL |
| 2015 | EZH2 plays a critical role in B-cell maturation and in non-Hodgkin’s lymphoma: Interplay between EZH2 function and B-cell activation | EZH2 (tazemetostat) | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | EZH2 plays a critical role in B-cell maturation and in non-Hodgkin’s lymphoma: Interplay between EZH2 function and B-cell activation |
| 2020 | Genetic and evolutionary patterns of treatment resistance in relapsed B-cell lymphoma | General | Blood Advances | Genetic and evolutionary patterns of treatment resistance in relapsed B-cell lymphoma |
| 2017 | Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma | CARM1 | Scientific Reports | Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma |
| 2014 | Identification of a First-In-Class PRMT5 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Mantle Cell Lymphoma | PRMT5 | American Society of Hematology (ASH) | Identification of a First-In-Class PRMT5 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Mantle Cell Lymphoma |
| 2018 | Identification of a peptide inhibitor for the histone methyltransferase WHSC1 | WHSC1 | PLoS One | Identification of a peptide inhibitor for the histone methyltransferase WHSC1 |
| 2015 | Identification of biomarkers and pathways associated with response to DOT1L inhibitor Pinometostat (EPZ-5676) in MLL-r leukemia | DOT1L | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | Identification of biomarkers and pathways associated with response to DOT1L inhibitor Pinometostat (EPZ-5676) in MLL-r leukemia |
| 2019 | Immunologic Correlates of the Abscopal Effect in a SMARCB1/INI1-negative Poorly Differentiated Chordoma after EZH2 Inhibition and Radiotherapy | EZH2 (tazemetostat) | Clinical Cancer Research | Immunologic Correlates of the Abscopal Effect in a SMARCB1/INI1-negative Poorly Differentiated Chordoma after EZH2 Inhibition and Radiotherapy |
| 2015 | Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis | General | Analytical Biochemistry | Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis |
| 2017 | Initial testing (stage 1) of tazemetostat (EPZ-6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program | EZH2 (tazemetostat) | Pediatric Blood & Cancer | Initial testing (stage 1) of tazemetostat (EPZ-6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program |
| 2017 | Interim Efficacy and Safety Data of Tazemetostat in Follicular Lymphoma and DLBCL from Ongoing Phase 2 Study | EZH2 (tazemetostat) | International Conference on Malignant Lymphoma (ICML) | Interim Efficacy and Safety Data of Tazemetostat in Follicular Lymphoma and DLBCL from Ongoing Phase 2 Study |
| 2018 | Interim Update of Tazemetostat in Follicular Lymphoma from Ongoing Phase 2 Study | EZH2 (tazemetostat) | European Hematology Association (EHA) | Interim Update of Tazemetostat in Follicular Lymphoma from Ongoing Phase 2 Study |
| 2015 | Loss of BAP1 function leads to EZH2-dependent transformation | General | Nature Medicine | Loss of BAP1 function leads to EZH2-dependent transformation |
| 2018 | Mechanism of action of synergistic activity of EZH2 inhibition and IMiDs® in preclinical multiple myeloma models | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | Mechanism of action of synergistic activity of EZH2 inhibition and IMiDs® in preclinical multiple myeloma models |
| 2017 | Mechanisms of Pinometostat (EPZ-5676) Treatment-Emergent Resistance in MLL-Rearranged Leukemia | DOT1L | Molecular Cancer Therapeutics | Mechanisms of Pinometostat (EPZ-5676) Treatment-Emergent Resistance in MLL-Rearranged Leukemia |
| 2016 | Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human | DOT1L | Cancer Chemotherapy and Pharmacology | Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human |
| 2013 | Molecular pathways: protein methyltransferases in cancer | General | Clinical Cancer Research | Molecular pathways: protein methyltransferases in cancer |
| 2019 | Natural History Study Poster EHA 2019 | EZH2 (tazemetostat) | European Hematology Association (EHA) | Natural History Study Poster EHA 2019 |
| 2014 | Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor | DOT1L | Biopharmaceutics & Drug Disposition | Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor |
| 2015 | Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor | SMYD3 | ACS Medicinal Chemistry Letters | Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor |
| 2018 | Opportunity for Therapeutic Expansion in Mantle Cell Lymphoma: Tazemetostat Combination Synergy Status in Preclinical MCL Models | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | Opportunity for Therapeutic Expansion in Mantle Cell Lymphoma: Tazemetostat Combination Synergy Status in Preclinical MCL Models |
| 2020 | Overcoming Immune Checkpoint Blockade Resistance via EZH2 Inhibition | EZH2 | Trends in Immunology | Overcoming Immune Checkpoint Blockade Resistance via EZH2 Inhibition |
| 2016 | Physiologically Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development | General | Drug Metabolism and Disposition | Physiologically Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development |
| 2015 | Pinometostat, EPZ-5676, Enhances the Anti-Proliferative Activity of MAP Kinase Pathway Inhibitors in Cell Lines Less Sensitive to DOT1L inhibition | DOT1L | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | Pinometostat, EPZ-5676, Enhances the Anti-Proliferative Activity of MAP Kinase Pathway Inhibitors in Cell Lines Less Sensitive to DOT1L inhibition |
| 2013 | Potent inhibition of DOT1L as a treatment for MLL-fusion leukemia | DOT1L | Blood | Potent inhibition of DOT1L as a treatment for MLL-fusion leukemia |
| 2016 | PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease | EZH2 | Biochemistry | PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease |
| 2015 | PRECLINICAL and CLINICAL EVALUATION OF EZH2 INHIBITORS IN MODELS OF SMALL CELL CARCINOMA OF THE OVARY, HYPERCALCEMIC TYPE (SCCOHT) | EZH2 (tazemetostat) | American Association for Cancer Research, National Cancer Institute, European Organisation for Research and Treatment of Cancer (AACR, NCI, EORTC) | PRECLINICAL and CLINICAL EVALUATION OF EZH2 INHIBITORS IN MODELS OF SMALL CELL CARCINOMA OF THE OVARY, HYPERCALCEMIC TYPE (SCCOHT) |
| 2014 | Preclinical Evaluation of EZH2 Inhibitors in Models of Human Synovial Sarcoma | EZH2 (tazemetostat) | National Center for Biotechnology Information | Preclinical Evaluation of EZH2 Inhibitors in Models of Human Synovial Sarcoma |
| 2016 | Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma | General | PLoS One | Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma |
| 2017 | Preliminary Evidence of Molecular Predictors of Tazemetostat in NHL | EZH2 (tazemetostat) | International Conference on Malignant Lymphoma (ICML) | Preliminary Evidence of Molecular Predictors of Tazemetostat in NHL |
| 2015 | Preliminary Report of the Phase 1 Study of the DOT1L Inhibitor Pinometostat (EPZ-5676) in Children with MLL-r Acute Leukemia: Safety, Exposure and Evidence of Target Inhibition | DOT1L | American Society of Hematology (ASH) | Preliminary Report of the Phase 1 Study of the DOT1L Inhibitor Pinometostat (EPZ-5676) in Children with MLL-r Acute Leukemia: Safety, Exposure and Evidence of Target Inhibition |
| 2011 | Promoting illiteracy in epigenetics: an emerging therapeutic strategy | General | Current Chemical Genomics and Translational Medicine | Promoting illiteracy in epigenetics: an emerging therapeutic strategy |
| 2018 | Protein methyltransferase inhibitors as precision cancer therapeutics: a decade of discovery | General | Philosophical Transactions of The Royal Society B | Protein methyltransferase inhibitors as precision cancer therapeutics: a decade of discovery |
| 2009 | Protein methyltransferases as a target class for drug discovery | General | Nature Reviews Drug Discovery | Protein methyltransferases as a target class for drug discovery |
| 2016 | Protein Methyltransferases: A Distinct, Diverse, and Dynamic Family of Enzymes | General | Biochemistry | Protein Methyltransferases: A Distinct, Diverse, and Dynamic Family of Enzymes |
| 2018 | Quantitative cell-based assay platform for assessment of combinatorial activity of the EZH2 inhibitor tazemetostat in multiple myeloma | EZH2 (tazemetostat) | Society for Laboratory Automation and Screening (SLAS) | Quantitative cell-based assay platform for assessment of combinatorial activity of the EZH2 inhibitor tazemetostat in multiple myeloma |
| 2014 | Reaction coupling between wild-type and disease-associated mutant EZH2 | EZH2 | ACS Chemical Biology | Reaction coupling between wild-type and disease-associated mutant EZH2 |
| 2020 | Real-world outcomes of patients with locally advanced or metastatic epithelioid sarcoma | EZH2 (tazemetostat) | Cancer | Real-world outcomes of patients with locally advanced or metastatic epithelioid sarcoma |
| 2014 | Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2 Mutant Non-Hodgkin Lymphoma | EZH2 (tazemetostat) | Molecular Cancer Therapeutics | Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2 Mutant Non-Hodgkin Lymphoma |
| 2011 | Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor | DOT1L | Cancer Cell | Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor |
| 2017 | Selective Killing of SMARCA2- and SMARCA4-Deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models | EZH2 | American Association for Cancer Research (AACR) | Selective Killing of SMARCA2- and SMARCA4-Deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models |
| 2018 | Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation | SMYD2 | PLoS One | Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation |
| 2015 | Small molecule inhibitors of EZH2: the emerging translational landscape | EZH2 | Epigenomics | Small molecule inhibitors of EZH2: the emerging translational landscape |
| 2015 | Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor | PRMT5 | Xenobiotica | Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor |
| 2015 | Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652 | PRMT | Drug Metabolism and Disposition | Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652 |
| 2016 | Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates | CARM1 | ACS Chemical Biology | Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates |
| 2015 | Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666 | PRMT5 | ACS Medicinal Chemistry Letters | Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666 |
| 2014 | Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas | EZH2 | PLoS One | Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas |
| 2010 | Targeting epigenetic enzymes for drug discovery | General | Current Opinion in Chemical Biology | Targeting epigenetic enzymes for drug discovery |
| 2013 | Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics | General | Oncogene | Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics |
| 2017 | Tazemetostat displays synergistic antiproliferative activity with backbone therapies in preclinical models of AT/RT and MRT | EZH2 (tazemetostat) | American Association for Cancer Research (AACR) | Tazemetostat displays synergistic antiproliferative activity with backbone therapies in preclinical models of AT/RT and MRT |
| 2016 | Tazemetostat Early Phase 2 NHL Study Findings at ASH Lymphoma | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Tazemetostat Early Phase 2 NHL Study Findings at ASH Lymphoma |
| 2016 | Tazemetostat Early Phase 2 NHL Study Findings Poster at ASH Lymphoma | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Tazemetostat Early Phase 2 NHL Study Findings Poster at ASH Lymphoma |
| 2020 | Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial | EZH2 (tazemetostat) | Lancet Oncology | Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial |
| 2020 | Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study | EZH2 (tazemetostat) | Lancet Oncology | Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study |
| 2016 | Tazemetostat Phase 1 NHL Update at ASH Lymphoma | EZH2 (tazemetostat) | American Society of Hematology (ASH) | Tazemetostat Phase 1 NHL Update at ASH Lymphoma |
| 2018 | Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study | EZH2 (tazemetostat) | Lancet Oncology | Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study |
| 2018 | The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia | DOT1L | Blood | The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia |
| 2016 | The drug-target residence time model: a 10-year retrospective | General | Nature Reviews Drug Discovery | The drug-target residence time model: a 10-year retrospective |
| 2010 | The dynamics of drug-target interactions: drug-target residence time and its impact on efficacy and safety | General | Expert Opinion on Drug Discovery | The dynamics of drug-target interactions: drug-target residence time and its impact on efficacy and safety |
| 2018 | The Elements of Translational Chemical Biology | General | Cell Chemical Biology | The Elements of Translational Chemical Biology |
| 2016 | The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat | EZH2 (tazemetostat) | Journal of Medicinal Chemistry | The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat |
| 2011 | The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states | EZH2 | FEBS Letters | The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states |
| 2017 | Selective Killing of SMARCA2- and SMARCA4-Deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models | EZH2 | Molecular Cancer Therapeutics | Selective Killing of SMARCA2- and SMARCA4-Deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models |
| 2021 | Results of the Phase 1b Soft-Tissue Sarcoma Port ion of the Global, Randomized, Double-Blind, Placebo-Controlled Study of Tazemetostat Plus Doxorubicin as Frontline Therapy for Advanced Epithelioid Sarcoma | EZH2 (tazemetostat) | American Society of Clinical Oncology (ASCO) | Results of the Phase 1b Soft-Tissue Sarcoma Port ion of the Global, Randomized, Double-Blind, Placebo-Controlled Study of Tazemetostat Plus Doxorubicin as Frontline Therapy for Advanced Epithelioid Sarcoma |
