EZH2 Drives Prostate Cancers

Epigenetic dysregulation is a hallmark of cancer cells.

Enhancer of zeste homolog 2 (EZH2) is an epigenetic and histone methyltransferase regulator. Prostate cancer patients with higher expression of the EZH2 gene are associated with a worse prognosis.

EZH2 drives prostate cancer growth and treatment resistance in a number of ways including:

  • Silencing tumor suppressor genes
  • Activating androgen receptor (AR) genes
  • Methylating non-histone targets

EZH2 is considered to be a novel target for cancer treatment.

Mevrometostat

Investigational mevrometostat is a selective, and orally bioavailable inhibitor of the protein (EZH2).

In prostate cancer, mevrometostat has demonstrated synergistic effects when combined with enzalutamide that may delay or prevent the emergence of enzalutamide-resistant NEPC state.

Mevrometostat + enzalutamide may restore gene functions repressed by both EZH2 and androgen receptors, resulting in downregulation of proliferation, survival, and cell cycle progression.

 

Watch this video to learn more about mevrometostat

Mevrometostat is investigational and not approved by any health authority.

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