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针对固体瘤正在研究的KAT6抑制剂:临床前和早期阶段的进展

Toru Mukohara¹

¹Department of Medical Oncology, National Cancer Center Hospital East, Kashiwa, Japan.

Expert opinion on investigational drugs

|February 17, 2026

概括

像Pifetrastat这样的KAT6抑制剂在治疗晚期乳腺癌和其他固体瘤方面表现有前途. 进一步的研究将探索它们的临床意义和更广泛应用的潜力.

科学领域:

在瘤学瘤学.
分子生物学分子生物学
表观遗传学在表观遗传学中,表观遗传学是指表观遗传学.

背景情况:

KAT6A和KAT6B (KAT6) 是MYST家族的基酸转移酶.
KAT6通过基因素H3乙化调节细胞过程.
在固体瘤中,KAT6A过度表达;在ER+乳腺癌中,KAT6对ESR1转录至关重要.

研究的目的:

为了评估KAT6抑制剂的临床意义,特别是Prifetrastat.
探索KAT6抑制剂在各种乳腺癌亚型和其他固体瘤中的应用.
制定策略来管理诸如失血症之类的副作用,并确定可预测生物标志物.

主要方法:

在ER+乳腺癌患者中进行Prifetrastat的I期试验.
在高级ER+乳腺癌中,Prifetrastat与Fulvestrant结合的III期试验.
各种KAT6催化抑制剂和降解剂的临床前和临床开发.

主要成果:

在第一阶段试验中, Prifetrastat 显示出有前途的疗效和良好的安全性概况,显着的副作用是异质症.
目前正在进行的III期试验预计将提供关于Prifetrastat临床影响的关键数据.
许多KAT6抑制剂正在临床前和临床开发中取得进展.

结论:

KAT6抑制剂代表了ER+晚期乳腺癌和潜在的其他固体瘤的有前途的治疗策略.
未来的研究应该专注于扩大KAT6抑制剂的应用,管理副作用,并开发反应生物标志物.
研究KAT6A选择性和KAT6/7抑制剂可能会揭示不同的疗效和安全性,从而推进KAT6向治疗.

关键词:

乳腺癌是什么? 乳腺癌是什么?它是HER2阴性的.在 KAT6AT6 中.PF07248144 是一个很好的方法.国家元首是国家元首.具有激素受体阳性的人.

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