mevrometostat + enzalutamide

**mevrometostat + enzalutamide** is an experimental combination therapy for metastatic castration-resistant prostate cancer (mCRPC). - **Mevrometostat** (PF-06821497) is a potent, selective inhibitor of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase involved in epigenetic repression and lineage plasticity, which can mediate androgen receptor (AR) signaling and promote resistance to AR pathway inhibitors[3]. - **Enzalutamide** is a nonsteroidal antiandrogen that selectively and competitively inhibits the AR, blocking androgen binding, nuclear translocation, and DNA interaction, and leading to suppression of androgen-dependent tumor growth[2][4]. The combination targets both epigenetic drivers of resistance (EZH2) and the androgen receptor pathway, aiming to extend clinical response and delay antiandrogen resistance. Clinical data from phase 1/2 and ongoing phase 3 trials show the combination significantly extends progression-free survival compared to enzalutamide alone in mCRPC patients previously treated with abiraterone[1][3][5].

Brand names

Xtandi (for enzalutamide)

Other names

combination mevrometostat/enzalutamide