tulmimetostat + enzalutamide

Tulmimetostat + enzalutamide is an investigational, oral combination drug regimen under clinical evaluation for metastatic castration-resistant prostate cancer (mCRPC). Tulmimetostat (CPI-0209) is a next-generation, dual inhibitor of Enhancer of Zeste Homolog 2 (EZH2) and EZH1. EZH2 is a histone methyltransferase and part of the Polycomb Repressive Complex 2 (PRC2); its inhibition reduces repressive methylation marks on DNA, reactivating suppressor genes and inhibiting tumor cell proliferation[2][8][7]. Enzalutamide is an androgen receptor antagonist that blocks androgen receptor nuclear translocation, DNA binding, and coactivator recruitment, inhibiting androgen-driven tumor growth[3]. This combination is developed for patients with mCRPC, including those post-abiraterone, and demonstrates additive activity with progression-free survival benefits over enzalutamide alone in phase 1/2 trials[1][4][6].

Brand names

XTANDI (enzalutamide)

Other names

tulmimetostat + enzalutamideCPI-0209 + enzalutamide