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Targeting Lineage Plasticity in Prostate Cancer with EZH2 Inhibitor Mevrometostat

By April 3, 2025No Comments

Oliver Sartor hosts Michael Schweizer to discuss mevrometostat. Dr. Schweizer explains this EZH2 inhibitor targets lineage plasticity and regulates androgen receptor activity, potentially overcoming resistance to standard treatments. The randomized study in metastatic castration-resistant prostate cancer patients who progressed on abiraterone showed impressive results – adding mevrometostat to enzalutamide reduced progression risk by 49%, extending median progression-free survival from 6 to 14 months. Though GI toxicities were common, only one patient discontinued treatment. A food effect study found lower doses with food maintained efficacy while significantly reducing side effects. This promising approach has launched two global phase III trials (MEVPRO-1 and MEVPRO-2), with potential implications beyond ARPI combinations, including possible synergies with immunotherapies and other novel treatment approaches.