使用静脉闭塞整体镜来评估血管效应:一项使用布洛克西布提德 (bloxibutid) 的研究,该药是一种血管激素II型2受体激动剂
Erik Rein-Hedin1,2, Folke Sjöberg1,3, Cecilia Ganslandt4
1CTC Clinical Trial Consultants AB, Uppsala, Sweden.
Clinical and translational science
|February 12, 2024
概括
布洛西布提德是一种血管激素II型2受体激动剂,在健康的志愿者中增加了前臂血流. 这表明对内皮功能障碍的潜在有效性,静脉封闭囊造影证明是一种有用的安全评估工具.
科学领域:
- 药理学 药理学是指药理学的学科.
- 心血管研究研究心血管研究
- 药物开发 药物开发
背景情况:
- 布洛西布提德 (C21) 是一种正在开发用于纤维化肺部疾病的血管新生素II型2受体 (AT2R) 激动剂.
- 研究新型AT2R激动剂对血管的影响对于了解它们的治疗潜力至关重要.
研究的目的:
- 在健康的男性中评估动脉内布洛克西布提德输液对血管的药理学影响.
- 评估动脉内布洛克西布提德的安全性和耐受性.
主要方法:
- 一期,开放标签,药学动力学研究,涉及五名健康的男性志愿者.
- 布洛克西布提德 (3-200μg/分钟) 的升高的动脉内剂量,给前臂.
- 前臂血流量 (FBF) 通过静脉封闭囊造影测量;用酸作为阳性对照.
主要成果:
- 布洛西布提德输液以剂量依赖的方式增加了FBF,最高剂量增加最大 (60.5%).
- 与基线相比,酸尼特显著增加了FBF (230-320%).
- 血压没有临床相关的变化;报告了与布洛克西布提德无关的三起轻度不良事件.
结论:
- 动脉内布洛西布提德增加了前臂的血液流动,这表明在内皮功能障碍的条件下具有潜在的实用性.
- 静脉闭塞整体镜是一种有效的方法来评估AT2R激动剂的血管效应和安全性.
- 布洛西布提德在本次急性动脉内给药研究中显示出有利的安全性.
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