优化早期临床药理学评估,以加快Giredestrant在晚期乳腺癌中的临床发展
Vikram Malhi1, Priya Agarwal1, Mary R Gates2
1Clinical Pharmacology, Genentech, Inc., South San Francisco, California.
Cancer research communications
|November 29, 2023
概括
吉雷德斯特兰在首次对人类进行的乳腺癌研究中显示了快速吸收和剂量相称的暴露. 这项试验的临床药理学数据将加速瘤学药物开发.
科学领域:
- 在瘤学瘤学.
- 临床药理学 临床药理学
- 药物开发 药物开发
背景情况:
- 雌激素受体阳性,HER2阴性局部晚期/转移性乳腺癌仍然是一个重要的治疗挑战.
- 吉雷德斯特兰 (Giredestrant) 是一种针对该患者群体的研究药物.
研究的目的:
- 描述giredestrant在首次人体研究中的临床药理学.
- 为了评估单剂giredestrant和与palbociclib结合的giredestrant的安全性,药理动力学,药理动力学和初步抗瘤活性.
主要方法:
- 一阶段Ia/Ib剂量升级/扩展研究 (NCT03332797).
- 剂量范围:10-250毫克每天一次用于单剂giredestrant.
- 组合治疗:吉雷德斯特兰100毫克与Palbociclib125毫克.
主要成果:
- 吉雷德斯特兰显示了快速吸收和与剂量成比例的暴露 (10-250毫克).
- 观察到最小的脏分泌和低CYP3A诱导潜力.
- 没有临床显著的药物相互作用与palbociclib;食物对暴露没有影响.
结论:
- 集成到早期阶段试验中的临床药理学特征说明了后期阶段的研究设计.
- 了解giredestrant的属性可以加速瘤药物开发,并优化试验设计.
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