Tulmimetostat is a selective and orally bioavailable Enhancer of Zeste Homolog 2 (EZH2) inhibitor, that demonstrates promising potential in treating hematologic malignancies and solid tumors.

To expand further research, we have created a set of analogs for Tulmimetostat.

EZH2 enzyme is a critical component of the polycomb repressive complex 2 (PRC2), which plays a key role in gene silencing through histone methylation. By inhibiting EZH2, Tulmimetostat reactivates the expression of tumor suppressor genes and inhibits cancer cell proliferation. In September 2023, the U.S. Food and Drug Administration granted Fast Track designation to Tulmimetostat for treating advanced, recurrent, or metastatic endometrial cancer with ARID1A mutations. In clinical trials, tulmimetostat has shown preliminary anti-tumor activity in patients with solid tumors and lymphomas. 

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