EZH2 Inhibitors
1 drugsAbout EZH2
EZH2 (Enhancer of Zeste Homolog 2) is a histone methyltransferase that modifies histone proteins by adding methyl groups, silencing gene expression. This epigenetic modification plays a crucial role in gene regulation and chromatin structure.
EZH2 is a compelling oncology drug target because aberrant activity can lead to uncontrolled cell growth. Currently, there is no genetic evidence directly linking EZH2 to specific diseases.
EZH2 is targeted by one FDA-approved small molecule drug, TAZVERIK, developed by EPIZYME INC for oncology indications. TAZVERIK was first approved in 2020.
Top EZH2 Drugs
EPIZYME INC is the only company with an approved drug targeting EZH2.
Low competition suggests a high barrier to entry or limited market attractiveness.
EZH2 Drug Modality Landscape
Modalities
Routes of Administration
Only one approved drug targets EZH2, using small molecule modality.
The lack of diverse modalities represents a whitespace opportunity for antibody or PROTAC development.
EZH2 Clinical Trials 49 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on EZH2. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 29 | 6 | 11 | 12 | 35% |
| Phase 2 | 19 | 7 | 5 | 6 | 58% |
| Phase 3 | 1 | 0 | 0 | 1 | - |
Top Sponsors
By Modality
Top Conditions
Top Drugs
EZH2 Drug Approval Timeline (2020 - 2020)
TAZVERIK was the first and only drug approved in 2020.
The single approval suggests the target is not yet saturated, but further approvals are needed to confirm trajectory.
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Competitive Landscape
- • 1 companies competing
- • Market share by company
Full Drug Portfolio
- • All 1 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 1-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 26 (6 companies)
- • Completion rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Count Trials
- Trials: phase 1-4 interventional trials on ClinicalTrials.gov that started in 2008 or later and test an FDA-approved drug acting on EZH2. A trial counts if an approved drug acting on EZH2 is in any arm, including as a comparator, and a trial that tests two such drugs counts once. Trials that test only unapproved drugs are not counted. A trial listed as phase 1/2 counts as phase 1, and phase 2/3 as phase 2.
- Active: recruiting, not yet recruiting, enrolling by invitation, or active and no longer recruiting.
- Completion rate: of the trials that have ended, the share marked Completed rather than Terminated or Withdrawn. Completed means the trial ended as planned; it does not mean the drug worked. Suspended trials are not counted as ended.
- Stopped: terminated or withdrawn. Trials stop for many reasons, including slow enrolment and business decisions, not only safety or efficacy.
- Sponsors: the lead sponsor of each trial. Companies are the sponsors ClinicalTrials.gov classes as industry; the rest are universities, hospitals, cooperative groups, government bodies and individuals.