Mevrometostat is an investigational new drug that is being evaluated by Pfizer for the treatment of metastatic castration‑resistant prostate cancer (mCRPC). It is a EZH2 histone methyltransferase inhibitor.
Pharmacology Mevrometostat has sub nanomolar affinity for the Y641N mutant form of EZH2 (which is a proliferation driver mutation). It also has low nanomolar inhibitory potency in reducing H3K27me3 levels and cellular proliferation in cells expressing the Y641N mutation.
Clinical trials Mevrometostat in combination with the androgen receptor antagonist enzalutamide in currently in a phase 3 clinical trial for treating advanced prostate cancer.
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