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An epigenetic drug that may re-sensitise prostate cancer to hormone therapy, in three phase 3 trials with enzalutamide.
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.
EZH2 inhibition reverses PRC2-mediated silencing and AR-independent lineage programmes. Connects to EZH2 and Androgen receptor.
1.Mevrometostat slips into a pocket on EZH2.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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Query for this drug: (TITLE:"Mevrometostat" OR ABSTRACT:"Mevrometostat" OR TITLE:"PF-06821497" OR ABSTRACT:"PF-06821497") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Mevrometostat, not a curated reading list.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Androgen receptor, Prostate cancer.
Shares Neuroendocrine and small-cell prostate cancer, EZH2, Lineage plasticity & neuroendocrine transformation, Androgen receptor.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Metastatic castration-resistant prostate cancer, Prostate cancer.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Neuroendocrine and small-cell prostate cancer, Lineage plasticity & neuroendocrine transformation, Androgen receptor, Metastatic castration-resistant prostate cancer.