Tag Archive for: EZH2 inhibitor

The MOMENT Trial: Mevrometostat Plus Enzalutamide in Post‑ARPI, Pre‑Abiraterone mCRPC

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Mevrometostat is an oral EZH2 inhibitor being developed to overcome resistance to androgen‑receptor–targeted therapy in prostate cancer. In tumors, EZH2 helps switch off tumor‑suppressor genes and supports androgen‑independent growth and lineage plasticity, changes that are strongly linked to progression on drugs like enzalutamide. Adding an EZH2 inhibitor to continued AR blockade is meant to “re‑discipline” […]

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HY809382: PRC2 Degrader Which Works With EZH2 Inhibitors Resistant Prostate Cancer

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Prostate cancer becomes especially hard to treat when it turns resistant to hormone therapies like enzalutamide, largely because of a protein complex called PRC2 that shuts down genes needed to fight tumors. PRC2’s key parts, EZH2 and EED, fuel cancer growth, immune evasion, and drug resistance in prostate tumors, as well as others like endometrial […]

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Igermetostat Plus Enzalutamide Delivers Promising rPFS in Post-Abiraterone mCRPC

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Igermetostat (XNW5004), a selective EZH2 inhibitor, pairs effectively with enzalutamide in metastatic castration-resistant prostate cancer after prior novel hormone therapy, based on phase 1b/2 results. EZH2 inhibition reverses enzalutamide resistance through epigenetic changes in castration-resistant prostate cancer models. The study endpoints focused on recommended phase 2 dose, safety, and radiographic progression-free survival. ​Eighty-four patients enrolled […]

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Phase 1/2 Trial: Valemetostat Plus Darolutamide in mCRPC

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A phase 1/2 clinical trial investigating valemetostat (DS-3201b), a dual EZH1/2 inhibitor, combined with darolutamide in metastatic castration-resistant prostate cancer (mCRPC) is going to start to recruit participants. This study aims to evaluate the safety, tolerability, and preliminary efficacy of the combination in men whose disease has progressed despite prior androgen receptor pathway inhibitors (ARPIs). […]

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Phase 2 Trial For a New Triplet Therapy: SHR3680 (Rezvilutamide), HS-20093 and SHR2554

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This Phase II study investigates the efficacy and safety of three investigational agents: SHR3680 (rezvilutamide), HS-20093, and SHR2554, aiming to enhance outcomes in metastatic prostate cancer through dual-pathway inhibition. SHR3680, a selective androgen receptor (AR) antagonist, represents the latest generation of hormonal therapy designed to inhibit the AR signaling axis, a critical driver of prostate […]

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