EZH2 inhibitor therapy for the treatment of androgen receptor mutation-induced prostate cancer

Combining an EZH2 inhibitor with enzalutamide effectively treats prostate cancer with AR mutations, addressing resistance issues in CRPC by enhancing progression-free survival and tumor reduction.

JP2026113667APending Publication Date: 2026-07-07CONSTELLATION PHARMA INC
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
CONSTELLATION PHARMA INC
Filing Date
2026-04-08
Publication Date
2026-07-07

AI Technical Summary

Technical Problem

Current treatments for castration-resistant prostate cancer (CRPC) are ineffective for most patients, with second-generation androgen receptor signaling inhibitors leading to rapid resistance, limiting treatment options and reducing progression-free survival.

Method used

Combining an EZH2 inhibitor, such as 7-chloro-2-(4-(3-methoxyazetidine-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridine-3-yl)methyl)benzo[d][1,3]dioxol-5-carboxamide, with an androgen receptor signaling inhibitor (ARSI) like enzalutamide to treat prostate cancer with AR mutations, enhancing progression-free survival and reducing tumor volume.

Benefits of technology

The combination therapy significantly increases progression-free survival by almost 2.5 times and demonstrates superior tumor volume reduction in prostate cancer models with pathogenic AR mutations compared to using ARSIs alone.

✦ Generated by Eureka AI based on patent content.

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Abstract

We provide treatment methods for prostate cancer. [Solution] A method is provided for treating prostate cancer having at least one pathogenic AR mutation, using 7-chloro-2-(4-(3-methoxyazetidine-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridine-3-yl)methyl)benzo[d][1,3]dioxol-5-carboxamide, or a pharmaceutically acceptable salt thereof, alone or in combination with a therapeutically effective dose of an androgen receptor signaling inhibitor (ARSI) such as enzalutamide.
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