Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) - Pipeline Review, H1 2018

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) - Pipeline Review, H1 2018


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Executive Summary

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Pipeline Review, H1 2018

Summary

According to the recently published report 'Histone Lysine N Methyltransferase EZH2-Pipeline Review, H1 2018'; Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) pipeline Target constitutes close to 17 molecules. Out of which approximately 16 molecules are developed by companies and remaining by the universities/institutes.

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Enhancer of zeste homolog 2 (EZH2) is a histone-lysine N-methyltransferase enzyme encoded by EZH2 gene. EZH2 methylates non-histone proteins such as the transcription factor GATA4 and the nuclear receptor RORA. It regulates the circadian clock via histone methylation at the promoter of the circadian genes. It is essential for the CRY1/2-mediated repression of the transcriptional activation of PER1/2 by the CLOCK-ARNTL/BMAL1 heterodimer, involved in the di and trimethylation of Lys-27 of histone H3 on PER1/2 promoters which is necessary for the CRY1/2 proteins to inhibit transcription.

The report 'Histone Lysine N Methyltransferase EZH2-Pipeline Review, H1 2018' outlays comprehensive information on the Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) targeted therapeutics, complete with analysis by indications, stage of development, mechanism of action (MoA), route of administration (RoA) and molecule type; that are being developed by Companies / Universities.

It also reviews key players involved in Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) targeted therapeutics development with respective active and dormant or discontinued projects. Currently, The molecules developed by companies in Phase II, Phase I, Preclinical and Discovery stages are 2, 2, 5 and 7 respectively. Similarly, the universities portfolio in Preclinical stages comprises 1 molecules, respectively.

Report covers products from therapy areas Oncology and Undisclosed which include indications Lymphoma, Diffuse Large B-Cell Lymphoma, Multiple Myeloma (Kahler Disease), Non-Hodgkin Lymphoma, Follicular Lymphoma, Small-Cell Lung Cancer, Solid Tumor, Acute Lymphocytic Leukemia (ALL, Acute Lymphoblastic Leukemia), Breast Cancer, Chondrosarcoma, Chordoma, Endometrial Cancer, Epithelial Tumor, Hematological Tumor, Hepatocellular Carcinoma, Hormone Refractory (Castration Resistant, Androgen-Independent) Prostate Cancer, Lung Cancer, Malignant Mesothelioma, Mantle Cell Lymphoma, Melanoma, Metastatic Hormone Refractory (Castration Resistant, Androgen-Independent) Prostate Cancer, Metastatic Liver Cancer, Metastatic Melanoma, Metastatic Transitional (Urothelial) Tract Cancer, Neuroblastoma, Non-Small Cell Lung Cancer, Ovarian Cancer, Peripheral Nerve Sheath Tumor (Neurofibrosarcoma), Peritoneal Cancer, Primary Mediastinal B-Cell Lymphoma, Prostate Cancer, Refractory Acute Myeloid Leukemia, Relapsed Acute Myeloid Leukemia, Renal Cell Carcinoma, Rhabdomyosarcoma, Soft Tissue Sarcoma, Squamous Non-Small Cell Lung Cancer, Synovial Sarcoma and Uterine Cancer.

Note: Certain content / sections in the pipeline guide may be removed or altered based on the availability and relevance of data.

Scope

- The report provides a snapshot of the global therapeutic landscape for Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)

- The report reviews Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) targeted therapeutics under development by companies and universities/research institutes based on information derived from company and industry-specific sources

- The report covers pipeline products based on various stages of development ranging from pre-registration till discovery and undisclosed stages

- The report features descriptive drug profiles for the pipeline products which includes, product description, descriptive MoA, R&D brief, licensing and collaboration details & other developmental activities

- The report reviews key players involved in Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) targeted therapeutics and enlists all their major and minor projects

- The report assesses Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) targeted therapeutics based on mechanism of action (MoA), route of administration (RoA) and molecule type

- The report summarizes all the dormant and discontinued pipeline projects

- The report reviews latest news and deals related to Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) targeted therapeutics

Reasons to buy

- Gain strategically significant competitor information, analysis, and insights to formulate effective R&D strategies

- Identify emerging players with potentially strong product portfolio and create effective counter-strategies to gain competitive advantage

- Identify and understand the targeted therapy areas and indications for Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)

- Identify the use of drugs for target identification and drug repurposing

- Identify potential new clients or partners in the target demographic

- Develop strategic initiatives by understanding the focus areas of leading companies

- Plan mergers and acquisitions effectively by identifying key players and it's most promising pipeline therapeutics

- Devise corrective measures for pipeline projects by understanding Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) development landscape

- Develop and design in-licensing and out-licensing strategies by identifying prospective partners with the most attractive projects to enhance and expand business potential and scope



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Table of Contents

List of Tables

List of Figures

Introduction

Global Markets Direct Report Coverage

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Overview

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Therapeutics Development

Products under Development by Stage of Development

Products under Development by Therapy Area

Products under Development by Indication

Products under Development by Companies

Products under Development by Universities/Institutes

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Therapeutics Assessment

Assessment by Mechanism of Action

Assessment by Route of Administration

Assessment by Molecule Type

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Companies Involved in Therapeutics Development

Daiichi Sankyo Co Ltd

Domainex Ltd

Epizyme Inc

GlaxoSmithKline Plc

Ionis Pharmaceuticals Inc

Kainos Medicine Inc

Pfizer Inc

Transgene Biotek Ltd

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Drug Profiles

CPI-1205-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

CPI-169-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

DS-3201-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

EBI-2554-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

GSK-343-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

IONISEZH-22.5Rx-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

JQEZ-5-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

KM-301-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

ORS-1-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

PF-06821497-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

Small Molecule to Inhibit EZH2 for Oncology-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

Small Molecules to Inhibit EZH2 for Oncology-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

Small Molecules to Inhibit EZH2 for Oncology-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

Small Molecules to Inhibit EZH2 for Solid Tumors-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

Small Molecules to Inhibit EZH2-EED for Oncology-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

tazemetostat-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

TBL-0404-Drug Profile

Product Description

Mechanism Of Action

R&D Progress

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Dormant Products

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Discontinued Products

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43)-Product Development Milestones

Featured News & Press Releases

Jun 03, 2018: Epizyme Presents Encouraging Phase 2 Data of Tazemetostat for Malignant Mesothelioma at ASCO

Jun 01, 2018: Epizyme to Host Investor Conference Call to Discuss Interim Follicular Lymphoma Clinical Data

May 17, 2018: Epizyme to Present New Tazemetostat Data at the American Society of Clinical Oncology (ASCO) Annual Meeting and the European Hematology Association Congress

Apr 23, 2018: Epizyme Provides Update Regarding Tazemetostat Clinical Program

Apr 09, 2018: Epizyme Announces Publication of Tazemetostat Phase 1 Clinical Data in The Lancet Oncology

Feb 09, 2018: Constellation Pharmaceuticals Announces Upcoming Presentation on its Anti-Neoplastic Drug Candidate CPI-1205

Jan 16, 2018: Constellation Pharmaceuticals Announces Initiation of Phase 1b/2 Study of CPI-1205

Dec 12, 2017: Constellation Pharmaceuticals Announces First Patient Dosed in Phase 1b/2 PROSTAR Combination Study of CPI-1205 in Advanced Form of Prostate Cancer

Dec 11, 2017: Daiichi Sankyo Presents Phase 1 Data for EZH1/2 Dual Inhibitor DS-3201 in Patients with Non-Hodgkin Lymphomas at the 59th Annual Meeting of the American Society of Hematology

Dec 10, 2017: Epizyme Presents New Biomarker Data on Tazemetostat at the American Society of Hematology Annual Meeting

Nov 14, 2017: Daiichi Sankyo Announces Presentation on its Investigational Agent DS-3201 at ASH

Nov 01, 2017: Epizyme Provides Update on Tazemetostat

Oct 27, 2017: Epizyme Presents Data from a Phase 1 Trial of Tazemetostat in Children with Relapsed or Refractory INI1-Negative Solid Tumors at the 2017 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

Jul 24, 2017: Epizyme Announces Tazemetostat to be Evaluated in NCI's Recently Initiated NCI-COG Pediatric MATCH Trial

Jun 21, 2017: Epizyme Announces Tazemetostat Granted Orphan Drug Designation for the Treatment of Soft Tissue Sarcoma

Appendix

Methodology

Coverage

Secondary Research

Primary Research

Expert Panel Validation

Contact Us

Disclaimer

List of Figures

Number of Products under Development by Stage of Development, H1 2018

Number of Products under Development by Therapy Areas, H1 2018

Number of Products under Development by Top 10 Indications, H1 2018

Number of Products by Stage and Mechanism of Actions, H1 2018

Number of Products by Stage and Route of Administration, H1 2018

Number of Products by Molecule Types, H1 2018

Number of Products by Stage and Molecule Types, H1 2018

List of Tables

Number of Products under Development by Stage of Development, H1 2018

Number of Products under Development by Therapy Areas, H1 2018

Number of Products under Development by Indications, H1 2018

Number of Products under Development by Indications, H1 2018 (Contd..1), H1 2018

Number of Products under Development by Companies, H1 2018

Products under Development by Companies, H1 2018

Products under Development by Companies, H1 2018 (Contd..1), H1 2018

Products under Development by Companies, H1 2018 (Contd..2), H1 2018

Products under Development by Companies, H1 2018 (Contd..3), H1 2018

Number of Products under Investigation by Universities/Institutes, H1 2018

Products under Investigation by Universities/Institutes, H1 2018

Number of Products by Stage and Mechanism of Actions, H1 2018

Number of Products by Stage and Route of Administration, H1 2018

Number of Products by Stage and Molecule Type, H1 2018

Pipeline by Daiichi Sankyo Co Ltd, H1 2018

Pipeline by Domainex Ltd, H1 2018

Pipeline by Epizyme Inc, H1 2018

Pipeline by GlaxoSmithKline Plc, H1 2018

Pipeline by Ionis Pharmaceuticals Inc, H1 2018

Pipeline by Kainos Medicine Inc, H1 2018

Pipeline by Pfizer Inc, H1 2018

Pipeline by Transgene Biotek Ltd, H1 2018

Dormant Projects, H1 2018

Discontinued Products, H1 2018

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Daiichi Sankyo Co Ltd

Domainex Ltd

Epizyme Inc

GlaxoSmithKline Plc

Ionis Pharmaceuticals Inc

Kainos Medicine Inc

Pfizer Inc

Transgene Biotek Ltd

Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) Therapeutic Products under Development, Key Players in Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) Therapeutics, Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) Pipeline Overview, Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) Pipeline, Histone Lysine N Methyltransferase EZH2 (ENX 1 or Enhancer Of Zeste Homolog 2 or Lysine N Methyltransferase 6 or EZH2 or EC 2.1.1.43) Pipeline Assessment

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