在晚期固体瘤和淋巴瘤中使用BET抑制剂OPN-2853:来自1b期PLX124-01试验的结果
Michael S Gordon1, Richard D Carvajal2,3, Alexander Spira4
1HonorHealth Research Institute, Scottsdale, AZ, USA.
Cancer chemotherapy and pharmacology
|March 5, 2026
概括
研究人员发现,布罗莫达因和外端 (BET) 抑制剂OPN-2853在患有晚期癌症的患者中耐受性良好. 推的第二阶段剂量为每日80毫克,显示适度的临床活性.
科学领域:
- 在瘤学瘤学.
- 药理学 药理学 是一个学科.
- 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:
- 基蛋白和外端蛋白 (BET) 是表观遗传调节剂,与各种癌症有关.
- OPN-2853 (扎瓦布雷西布) 是一种新型,强效的口服抑制剂,针对所有四种BET蛋白.
研究的目的:
- 为了确定OPN-2853.3的推第二阶段剂量 (RP2D).
- 评估OPN-2853在患有晚期固体瘤或非霍奇金淋巴瘤 (NHL) 的成年人中的安全性,药理动力学和药理动力学.
主要方法:
- 进行了第一次在人体上进行的开放标签第1b期研究.
- 主要终点包括RP2D,药理动力学和安全性.
- 二级和探索性终点侧重于疗效和药理动力学.
主要成果:
- 确定的RP2D是80毫克口服每天一次 (QD).
- 最常见的不良事件是恶心和疲劳;没有发生与治疗相关的死亡.
- 观察到两种已确认的客观反应,包括一个完全反应与18个月的无进展生存期.
结论:
- 在患有晚期固体瘤和NHL的患者中,OPN-2853在RP2D表现出良好的耐受性.
- 该研究确定了耐受性良好的剂量,并提供了关于OPN-2853.3临床活性的初步数据.
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