# Mevrometostat

Source: https://onco.cc/drugs/mevrometostat/  
OnCo record `mevrometostat` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

An epigenetic drug that may re-sensitise prostate cancer to hormone therapy, in three phase 3 trials with enzalutamide.

## Summary

Mevrometostat is an oral EZH2 inhibitor; blocking the methyltransferase reverses PRC2-mediated gene silencing and the AR-independent lineage programmes that let prostate cancer escape hormone therapy, which is intended to re-sensitise tumours to enzalutamide. In a phase 1/2 study after abiraterone, mevrometostat with enzalutamide gave rPFS of about 14 months versus 6 months with enzalutamide alone. Three phase 3 trials with enzalutamide are running: MEVPRO-1 (post-abiraterone mCRPC, open-label, about 600 men, started October 2024, completion around 2028), MEVPRO-2 (double-blind) and MEVPRO-3 (mCSPC, ASCO GU 2026 trial-in-progress). There is no approval yet, and whether the randomised trials confirm the early rPFS signal is the key question. For a newcomer, it is an epigenetic drug that may make hormone therapy work again.

## Fields

- Kind: Treatment
- Status: phase-3
- Last checked: 2026-09-06
- Code: PF-06821497
- Modality: Small-molecule EZH2 inhibitor
- Mechanism: EZH2 inhibition reverses PRC2-mediated silencing and AR-independent lineage programmes.

## Sources

- MEVPRO-1/2 protocols (Future Oncology 2026): https://www.tandfonline.com/doi/full/10.1080/14796694.2026.2667441

## Connected records

- cancers: [Metastatic castration-resistant prostate cancer](https://onco.cc/cancers/prostate-mcrpc/), [Neuroendocrine and small-cell prostate cancer](https://onco.cc/cancers/prostate-nepc/), [Prostate cancer](https://onco.cc/cancers/prostate/)
- technologies: [Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET)](https://onco.cc/technologies/epigenetic-drugs/)
- targets: [Androgen receptor](https://onco.cc/targets/androgen-receptor/), [EZH2](https://onco.cc/targets/ezh2/)
- companies: [Pfizer (incl. Seagen)](https://onco.cc/companies/pfizer/)
- trials: [A Study to Learn How PF-06821497 (Mevrometostat) Works in Men With Metastatic Castration-resistant Prostate Cancer.](https://onco.cc/trials/nct06629779/), [MEVPRO-1](https://onco.cc/trials/mevpro-1/), [This Study Will Explore Whether a Combination of the Investigational Drug Mevrometostat (PF-06821497) and Enzalutamide Will Work Better Than Taking En](https://onco.cc/trials/nct07028853/)
- ideas: [Unmask hidden antigens with a short epigenetic course before immunotherapy](https://onco.cc/ideas/idea-bio2-epigenetic-priming-cold-tumours/)
- pathways: [Lineage plasticity & neuroendocrine transformation](https://onco.cc/pathways/lineage-plasticity-neuroendocrine/)
- roadmaps: [Epigenetic therapy roadmap: loosening silenced genes → mutation-specific enzymes → editing the epigenome](https://onco.cc/roadmaps/epigenetics-roadmap/), [Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test](https://onco.cc/roadmaps/hormonal-therapy-roadmap/)

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