mevrometostat

Mevrometostat is an orally available, potent, and selective small molecule inhibitor of enhancer of zeste homolog 2 (EZH2), a histone lysine methyltransferase that acts as the catalytic subunit of the polycomb repressive complex 2 (PRC2). EZH2 plays a key role in epigenetic regulation by modifying gene expression patterns that control cell fate decisions such as differentiation and self-renewal. Mevrometostat inhibits both wild-type and mutant Y641N EZH2 with high specificity, leading to decreased H3K27 methylation and reactivation of gene expression for EZH2 target genes. The drug is being developed primarily for metastatic castration-resistant prostate cancer (mCRPC), where it has shown promising results in combination with enzalutamide and androgen deprivation therapy by improving radiographic progression-free survival compared to standard treatment alone. It is also under investigation for follicular lymphoma and small cell lung cancer.

Other names

PF 06821497PF06821497PF-06821497mevrometostat