The EZH2 inhibitor mevrometostat is moving into phase 3 trials as a potential treatment for metastatic castration-resistant prostate cancer after encouraging early results. The approach targets EZH2, an epigenetic regulator that helps cancer cells become more aggressive and resistant to treatment, including androgen receptor pathway inhibitors like enzalutamide.
In a phase 1 study, combining mevrometostat with enzalutamide improved outcomes compared with enzalutamide alone. Patients receiving the combination had longer progression-free survival and higher rates of PSA reduction. The treatment was generally well tolerated, with manageable side effects such as diarrhea, fatigue, taste changes, and anemia.
Two phase 3 trials, MEVPRO-1 and MEVPRO-2, are now underway to confirm these findings. One study focuses on patients who have already progressed on prior therapy, while the other evaluates the combination earlier in treatment. Researchers hope this strategy can restore sensitivity to hormonal therapy and delay the need for chemotherapy.