tazemetostat + enzalutamide

**tazemetostat + enzalutamide** is an investigational oral combination therapy for metastatic castration-resistant prostate cancer (mCRPC). It combines **tazemetostat**, a small molecule inhibitor of *histone-lysine N-methyltransferase EZH2*, with **enzalutamide**, a second-generation antiandrogen that blocks the *androgen receptor (AR)*. Tazemetostat prevents cancer cell de-differentiation by inhibiting EZH2-mediated histone H3K27 trimethylation, while enzalutamide inhibits AR by preventing androgen binding and nuclear translocation, thereby suppressing androgen-driven tumor growth. The rationale for combination is that EZH2 inhibition may help overcome resistance to AR signaling inhibitors in prostate cancer. This regimen is being evaluated for safety, tolerability, and preliminary efficacy in ongoing phase 1b/2 studies for patients previously treated with abiraterone/prednisone or enzalutamide[1][3][5].

Brand names

None known for the combination; individual drugs are brand-named Tazverik (tazemetostat) and Xtandi (enzalutamide)