tulmimetostat

Tulmimetostat is an orally available, next-generation small molecule inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 2 (EZH2) and enhancer of zeste homolog 1 (EZH1), which are catalytic subunits of the polycomb repressive complex 2 (PRC2)[1][6][7]. By selectively binding to and inhibiting EZH2 and EZH1, tulmimetostat prevents methylation of histone H3 on lysine 27 (H3K27), leading to altered gene expression patterns associated with cancer pathways. This results in decreased proliferation and survival of cancer cells that overexpress or harbor mutations in these enzymes[1][2][8]. Tulmimetostat has shown particular promise in preclinical models with ARID1A or BAP1 mutations. It is being developed as a potential treatment for various cancers including non-small cell lung cancer, mycosis fungoides, Sézary syndrome, endometrial carcinoma (especially ARID1A-mutated), ovarian clear cell carcinoma, diffuse large B-cell lymphoma, peripheral T-cell lymphoma, mesothelioma (BAP1-mutated), castration-resistant prostate cancer, bladder cancer and other solid tumors[5][6][7][8]. The drug is currently under investigation in Phase I/II clinical trials.

Other names

tulmimetostat [INN]