On November 4, 2015 Epizyme, Inc. (NASDAQ: EPZM), a clinical stage biopharmaceutical company creating novel epigenetic therapies for cancer patients, reported that it will present data from 11 accepted abstracts on the role of histone methyltransferase (HMT) inhibition in human cancers at the AACR (Free AACR Whitepaper)-NCI-EORTC AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper) taking place in Boston, Mass., November 5 – 9, 2015 (Press release, Epizyme, NOV 4, 2015, View Source [SID:1234507944]). Among the presentations are important new data on the critical role played by EZH2 in Non-Hodgkin Lymphoma (NHL). Epizyme’s lead compound, tazemetostat, is a first-in-class EZH2 inhibitor currently being studied in relapsed or refractory B-cell NHL and advanced solid tumors.
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"Epizyme is leading the field of epigenetic drug discovery with our focused approach to development of small molecule therapeutics against HMTs and other chromatin modifiers," said Robert A. Copeland, Ph.D., President of Research and Chief Scientific Officer. "Our presentations at the AACR (Free AACR Whitepaper)-NCI-EORTC meeting demonstrate the breadth of our drug discovery efforts and preclinical target identification in this space and our continued commitment to understanding the role of EZH2 and EZH2 inhibition across a spectrum of cancer indications."
Presentations on the role of EZH2 include:
EZH2 Plays a Critical Role in B-cell Maturation and in Non-Hodgkin Lymphoma: Interplay between EZH2 Function and B-cell Activation
Abstract number: B85
Speaker: Danielle Johnston, Epizyme, Inc.
Session title: Poster Session B, Epigenetic Targets
Presentation time: Saturday, November 7, 12:30 – 3:30
Advanced Image Analysis of H3K27 Trimethylation in Skin from Subjects Dosed with the EZH2 Inhibitor Tazemetostat
Abstract number: B6
Speaker: Alice McDonald, Epizyme, Inc.
Session title: Poster Session B, Biomarkers
Presentation time: Saturday, November 7, 12:30 – 3:30
EZH2 Inhibition Leads to Decreased Proliferation in SMARCA4-deleted Ovarian Cancer Cell Lines
Abstract number: C87
Speaker: Elayne Penebre, Epizyme, Inc.
Session title: Poster Session C, Epigenetic Targets
Presentation time: Sunday, November 8, 12:30 – 3:30
Initial Testing (Stage 1) of EPZ-6438 (tazemetostat), a Novel EZH2 Inhibitor, by the Pediatric Preclinical Testing Program (PPTP)
Abstract number: A137
Speaker: Raushan Kurmasheva, Greehey Children’s Cancer Research Institute
Session title: Poster Session A, Pediatric Early Drug Development
Presentation time: Friday, November 6, 12:15 – 3:15
Physiologically-based pharmacokinetic modeling to support clinical investigation of the EZH2 inhibitor, tazemetostat (EPZ-6438) in INI1-deficient pediatric tumors
Abstract number: A135
Speaker: Nigel Waters, Epizyme, Inc.
Session title: Poster Session A, Pediatric Early Drug Development
Presentation time: Friday, November 6, 12:15 – 3:15
Chromatin Flow Cytometry Based Quantification of Cell Type Specific Alterations in Histone Methylation States Resulting from in vitro and in vivo EZH2 Inhibitor Treatment
Abstract number: B133
Speaker: Christopher Plescia, Epizyme, Inc.
Session title: Poster Session B, Novel Assay Technology
Presentation time: Saturday, November 7, 12:30 – 3:30
In addition to these presentations on the role of EZH2, Epizyme will present additional data on the company’s ongoing work to elucidate the potential of HMT inhibitors as treatments for human cancers. These additional presentations include:
CRISPR Pooled Screening Identifies Differential Dependencies on Epigenetic Pathways
Abstract number: B78
Speaker: Alexandra R. Grassian, Epizyme, Inc.
Session title: Poster Session B, Epigenetic Targets
Presentation time: Saturday, November 7, 12:30 – 3:30
Pinometostat (EPZ-5676) Enhances the Anti-proliferative Activity of MAP Kinase Pathway Inhibitors in MLL-r Leukemia Cell Lines
Abstract number: B82
Speaker: Alejandra Raimondi, Epizyme, Inc.
Session title: Poster Session B, Epigenetic Targets
Presentation time: Saturday, November 7, 12:30 – 3:30
Identification of a Novel Potent Selective SMYD3 Inhibitor with Oral Bioavailability
Abstract number: C85
Speaker: Lorna Mitchell, Epizyme, Inc.
Session title: Poster Session C, Epigenetic Targets
Presentation time: Sunday, November 8, 12:30 – 3:30
Identification of Biomarkers and Pathways Associated with Response to the DOT1L Inhibitor Pinometostat (EPZ-5676) in MLL-r Leukemia
Abstract number: C12
Speaker: Scott Daigle, Epizyme, Inc.
Session title: Poster Session C, Biomarkers
Presentation time: Sunday, November 8, 12:30 – 3:30
A Medium-Throughput Single Cell CRISPR CAS9 Assay to Assess Gene Essentiality
Abstract number: C162
Speaker: Alexandra Grassian, Epizyme, Inc.
Session title: Poster Session C, Target Identification and Validation
Presentation time: Sunday, November 8, 12:30 – 3:30
About EZH2 in Cancer
EZH2 is a histone methyltransferase (HMT) that is increasingly understood to play a potentially oncogenic role in a number of cancers. These include Non-Hodgkin Lymphoma, INI1-deficient cancers such as malignant rhabdoid tumors, epithelioid sarcomas and synovial sarcoma, and a range of other solid tumors.
About Tazemetostat
Epizyme is developing tazemetostat for the treatment of patients with Non-Hodgkin Lymphoma and for patients with INI1-deficient solid tumors. Tazemetostat is a first-in-class small molecule inhibitor of EZH2 created by Epizyme using its proprietary product platform. In some human cancers, aberrant EZH2 enzyme activity results in misregulation of genes that control cell proliferation resulting in the rapid and unconstrained growth of tumor cells. Tazemetostat is the WHO International Non-Proprietary Name (INN) for compound EPZ-6438.
Additional information about this program, including clinical trial information, may be found here: View Source