I am a bit slow, I am in Poland for work so I have to carve in the time to post.
Mevrometostat (PF-06821497) is an experimental drug being investigated in a Phase III trial (NCT06551324) called MEVPRO-1.
This trial is for men with metastatic castration-resistant prostate cancer (mCRPC) who have received prior treatment with abiraterone acetate. Mevrometostat functions by inhibiting the enhancer of zeste homolog 2 (EZH2) protein, which plays a role in prostate cancer cell growth.
The drug targets H3K27Me3, a protein that suppresses cancer cell growth, and aims to overcome resistance to the androgen receptor pathway by targeting the mutated EZH2 protein, which can act as a co-activator for the androgen receptor. EZH2 is also believed to be a key driver of neuroendocrine prostate cancer, and mevrometostat may help prevent the differentiation of prostate cancer into this aggressive subtype.
The MEVPRO-1 study is expected to be completed in December 2025 and involves 600 patients across multiple sites in the US, Australia, and Asia. The primary endpoint of the study is radiographic progression-free survival (rPFS) for up to two years. Patients in the treatment arm receive mevrometostat twice daily along with daily enzalutamide, while the comparator arm receives either enzalutamide or docetaxel.