{"entity":{"id":"mevrometostat","kind":"drug","name":"Mevrometostat","aka":[],"tldr":"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.","status":"phase-3","asOf":"2026-09-06","links":[{"label":"MEVPRO-1/2 protocols (Future Oncology 2026)","url":"https://www.tandfonline.com/doi/full/10.1080/14796694.2026.2667441"}],"tags":[],"related":[],"cancers":["prostate","prostate-mcrpc"],"sections":[],"technologies":["epigenetic-drugs"],"targets":["ezh2","androgen-receptor"],"drugs":[],"companies":["pfizer"],"institutions":[],"pathways":[],"terms":[],"trials":["mevpro-1","nct06629779","nct07028853"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"PF-06821497","modality":"Small-molecule EZH2 inhibitor","mechanism":"EZH2 inhibition reverses PRC2-mediated silencing and AR-independent lineage programmes.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/mevrometostat/","neighbours":{"cancer":[{"id":"prostate-mcrpc","kind":"cancer","name":"Metastatic castration-resistant prostate cancer","route":"/cancers/prostate-mcrpc/"},{"id":"prostate-nepc","kind":"cancer","name":"Neuroendocrine and small-cell prostate cancer","route":"/cancers/prostate-nepc/"},{"id":"prostate","kind":"cancer","name":"Prostate cancer","route":"/cancers/prostate/"}],"technology":[{"id":"epigenetic-drugs","kind":"technology","name":"Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET)","route":"/technologies/epigenetic-drugs/"}],"target":[{"id":"androgen-receptor","kind":"target","name":"Androgen receptor","route":"/targets/androgen-receptor/"},{"id":"ezh2","kind":"target","name":"EZH2","route":"/targets/ezh2/"}],"company":[{"id":"pfizer","kind":"company","name":"Pfizer (incl. Seagen)","route":"/companies/pfizer/"}],"trial":[{"id":"nct06629779","kind":"trial","name":"A Study to Learn How PF-06821497 (Mevrometostat) Works in Men With Metastatic Castration-resistant Prostate Cancer.","route":"/trials/nct06629779/"},{"id":"mevpro-1","kind":"trial","name":"MEVPRO-1","route":"/trials/mevpro-1/"},{"id":"nct07028853","kind":"trial","name":"This Study Will Explore Whether a Combination of the Investigational Drug Mevrometostat (PF-06821497) and Enzalutamide Will Work Better Than Taking En","route":"/trials/nct07028853/"}],"idea":[{"id":"idea-bio2-epigenetic-priming-cold-tumours","kind":"idea","name":"Unmask hidden antigens with a short epigenetic course before immunotherapy","route":"/ideas/idea-bio2-epigenetic-priming-cold-tumours/"}],"pathway":[{"id":"lineage-plasticity-neuroendocrine","kind":"pathway","name":"Lineage plasticity & neuroendocrine transformation","route":"/pathways/lineage-plasticity-neuroendocrine/"}],"roadmap":[{"id":"epigenetics-roadmap","kind":"roadmap","name":"Epigenetic therapy roadmap: loosening silenced genes → mutation-specific enzymes → editing the epigenome","route":"/roadmaps/epigenetics-roadmap/"},{"id":"hormonal-therapy-roadmap","kind":"roadmap","name":"Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test","route":"/roadmaps/hormonal-therapy-roadmap/"}]}}