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By modulating critical gene expression, EZH2 promotes cell cycle progression, cell proliferation, differentiation, and apoptosis.1
EZH2 is overexpressed in several malignant tumors and recurrently mutated in other cancers.2 It provides a critical role in promoting tumor growth and metastasis and can be regulated through multiple pathways transcriptionally, post-transcriptionally, and post-translationally.2
Understanding the Role of EZH2
Expression in Cancer
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EZH2 Inhibitors
EZH2 inhibitors are anticancer drugs that target EZH2 enzymes and suppress their overactivity, thus slowing cell growth and inhibiting tumor formation. This table outlines therapies targeting EZH2 both approved by the FDA and in the pipeline.
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EZH2 Inhibitors Approved by the FDAa |
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Brand Name (Generic Drug Name) |
Indications |
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Tazverik (tazemetostat)1 |
Treatment of adults and pediatric patients aged ≥16 years with metastatic or locally advanced epithelioid sarcoma ineligible for complete resection |
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Treatment of adults with relapsed or refractory FL with EZH2 mutation detected by an FDA-approved test who have received ≥2 prior systemic therapies |
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Treatment of adults with relapsed or refractory FL who have no satisfactory alternative treatment options |
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EZH2 Inhibitors in the Pipelineb |
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Generic Drug Name |
Potential Indications |
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PF-068214972 |
Being evaluated for the treatment of patients with prostate cancer |
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EZH2, enhancer of zeste homolog 2; follicular lymphoma, FL.
aAdapted from prescribing information.1 b Adapted from manufacturer websites.2 |
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