Tulmimetostat

Tulmimetostat is a second-generation EZH2 inhibitor that has been designed to achieve comprehensive target coverage through extended on-target residence time.

EZH2 acts as an epigenetic writer and normally places one or more methyl groups on a histone protein, leading to the suppression of gene expression. Some cancers depend on an abnormal pattern of gene expression and re-direct EZH2 to genes that become abnormally repressed. Cancer cells with these abnormal gene expression programs may be more resistant to anti-cancer therapies.

Abnormal EZH2 function has been implicated in a number of ways in specific cancers, a finding that offers broad therapeutic potential for EZH2 inhibition:

• Synergy with oncogenic drivers in prostate cancer
• Activating mutations in lymphoma
• Tumor immunity in solid tumors
• Drug resistance in solid tumors
• Synthetic lethality in genetically defined solid tumors

Tulmimetostat has demonstrated more potent anti-tumor activity compared with first-generation EZH2 inhibitors in preclinical models of multiple cancer types. It does not induce its own metabolism, which has been an issue with other EZH2 inhibitors.

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