Cover Story: Chromatin's rising tide

Table 1. Select clinical-stage compounds that target epigenetic regulators. The availability of new research tools and data on epigenetic regulators has driven the development of a new wave of compounds. At least nine molecules have entered clinical trials since the start of 2013, including four BET bromodomain-targeting oncology programs. GlaxoSmithKline plc (LSE:GSK; NYSE:GSK) leads the pack with clinical-stage programs against three targets, while Celgene Corp. (NASDAQ:CELG) has rights or options to two programs.
Source: BCIQ; BioCentury Archives; ClinicalTrials.gov

Company

Compound

Description

Indication

Status

Resverlogix Corp. (TSX:RVX)

RVX-208

BET bromodomain inhibitor

Atherosclerosis

Phase II

Acetylon Pharmaceuticals Inc.; Celgene

Rocilinostat (ACY-1215)

Oral selective histone deacetylase 6 (HDAC6) inhibitor

Multiple myeloma (MM)

Phase I/II

Epizyme Inc. (NASDAQ:EPZM); Eisai Co. Ltd. (Tokyo:4523)

EPZ-6438

Enhancer of zeste homolog 2 (EZH2) inhibitor

Lymphomas including those with EZH2 mutations

Phase I/II

Oryzon Genomics S.A.; Roche (SIX:ROG; OTCQX:RHHBY)

ORY-1001

Lysine-specific demethylase 1 (KDM1A; LSD1) inhibitor

Acute myelogenous leukemia (AML)

Phase I/IIa

Constellation Pharmaceuticals Inc.

CPI-0610

BET bromodomain inhibitor

Lymphoma

Phase I

Epizyme; Celgene

EPZ-5676

Histone methyltransferase DOT1L (DOT1L) inhibitor

Myeloid-lymphoid or mixed-lineage leukemia (MLL; HRX)-rearranged leukemia

Phase I

GlaxoSmithKline

GSK2879552 

LSD1 inhibitor

Small cell lung cancer

Phase I

GSK525762

BET bromodomain inhibitor

Cancers including NUT midline carcinomas

Phase I

GSK2816126 

EZH2 inhibitor

Lymphomas including those with EZH2 mutations

Phase I

Oncoethix S.A.; Mitsubishi Tanabe Pharma Corp. (Tokyo:4508)

OTX015

BET bromodomain inhibitor

Hematologic malignancies

Phase I

Tensha Therapeutics Inc.

TEN-010

BET bromodomain inhibitor

Cancers including NUT midline carcinomas

Phase I