Investigational Drug
Mervometostat
TrialFetch AI Analysis
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Overview
Mervometostat (more commonly spelled mevrometostat; PF-06821497) is an investigational oral cancer drug. Human results have been reported from early-phase studies in follicular lymphoma and metastatic castration-resistant prostate cancer (mCRPC). Phase 3 prostate-cancer trials are underway; the results below do not establish a clinical benefit. (annalsofoncology.org)
Mechanism of action
Mevrometostat inhibits EZH2, an enzyme involved in repressing gene expression through methylation of histone H3. Reduced H3K27 methylation has been observed in samples from treated patients, providing evidence that the drug engages its target. (ascopubs.org)
Efficacy
In an 81-patient randomized phase 1 dose-expansion study of people with previously treated mCRPC, mevrometostat plus enzalutamide was compared with enzalutamide alone. Median radiographic progression-free survival was 14.3 versus 6.2 months. Among patients with measurable disease, objective responses occurred in 4/15 (26.7%) versus 2/14 (14.3%); confirmed PSA declines of at least 50% occurred in 34.1% versus 15.4%. These are preliminary findings from a small study, not phase 3 results. (meeting.neaua.org)
In an earlier phase 1 monotherapy cohort, 4 of 15 patients with follicular lymphoma had partial responses. (annalsofoncology.org)
Safety
In the randomized mCRPC study, grade 3 or higher treatment-emergent adverse events occurred in 53.7% receiving the combination and 42.5% receiving enzalutamide alone. Diarrhea was reported in 78.0% versus 15.0%, respectively; decreased appetite, altered taste, and anemia were also more frequent with the combination. No treatment-related deaths were reported. (meeting.neaua.org)
Further reading
- Randomized phase 1 dose-expansion results
- Earlier phase 1 results across follicular lymphoma, prostate cancer, and small-cell lung cancer
- Phase 3 MEVPRO-1 and MEVPRO-2 trial protocols
Last updated: Sep 2026
Active trials using Mervometostat
Found 4 active trials using this drug:
TrialFetch AI summary: Men with metastatic castration-sensitive prostate adenocarcinoma and ECOG performance status 0–1 who have not received an androgen receptor pathway inhibitor or chemotherapy for metastatic disease are randomized to enzalutamide plus mevrometostat or enzalutamide plus placebo. Mevrometostat is an investigational EZH2 inhibitor that reduces histone H3K27 methylation.
ClinicalTrials.gov ID: NCT07028853
TrialFetch AI summary: This trial enrolls patients with progressive metastatic castration-resistant prostate adenocarcinoma who have not received systemic treatment for mCRPC or prior enzalutamide, apalutamide, darolutamide, or abiraterone. Patients receive enzalutamide plus either mevrometostat, an investigational EZH2 inhibitor, or placebo.
ClinicalTrials.gov ID: NCT06629779
TrialFetch AI summary: Adults with metastatic castration-resistant prostate adenocarcinoma progressing after abiraterone, without prior enzalutamide or another next-generation androgen receptor inhibitor, are randomized to mevrometostat plus enzalutamide or physician’s choice of enzalutamide or docetaxel. Mevrometostat inhibits EZH2, an epigenetic enzyme involved in gene repression.
ClinicalTrials.gov ID: NCT06551324
TrialFetch AI summary: Adults with relapsed or refractory small-cell lung cancer, follicular lymphoma, or castration-resistant prostate cancer receive oral mevrometostat, an investigational EZH2 inhibitor, alone or with enzalutamide. A randomized metastatic prostate cancer cohort compares the combination with enzalutamide alone in patients previously treated with abiraterone but not enzalutamide or other specified androgen-receptor inhibitors.
ClinicalTrials.gov ID: NCT03460977
