小分子中性粒细胞调节器ADS051在第一阶段单个上升剂量研究中是安全且耐受良好的
Adam S Cheifetz1,2, Jessica R Allegretti1,3, Megan Quintas4
1Harvard Medical School, Boston, Massachusetts, USA.
The American journal of gastroenterology
|November 26, 2024
概括
新药ADS051在性结肠炎 (UC) 治疗方面表现有前途. 这种抑制中性粒细胞的药物是安全的,耐受性很好,并且在最小的全身暴露下在肠道中达到高度.
科学领域:
- 胃肠病学 胃肠病学
- 药理学 药理学是指药理学的学科.
- 免疫学 免疫学 免疫学
背景情况:
- 目前的性结肠炎 (UC) 治疗方法在有效性和安全性方面存在局限性.
- 中性粒细胞的转移和激活与UC病原和症状有关.
- ADS051是一种新型小分子,旨在抑制中性粒细胞迁移和激活.
研究的目的:
- 在健康志愿者中评估ADS051的安全性,耐受性和药理动力学.
- 通过检查其在胃肠道中的局部作用来评估ADS051作为UC治疗剂的潜力.
主要方法:
- 一个第一阶段,单次上升剂量研究,涉及50名健康成年人.
- 参与者被随机分为5个队伍,接受口服剂量的ADS051 (100毫克至3,500毫克) 或安慰剂.
- 在便,血液和尿液中的安全性,耐受性和药理动力学被监测了剂后30天.
主要成果:
- 在所有剂量组中,ADS051被发现是安全的和耐受性良好.
- 最常见的不良事件是便秘,在1,500毫克剂量的参与者中,5.0%的人报告了这种情况.
- 在便中发现ADS051的高度 (剂量的10%-24%),系统吸收最小 (仅在2个血液样本中可量化) 和尿液分泌低 (剂量的<0.035%).
结论:
- 在健康志愿者中,ADS051表现出良好的安全性和耐受性.
- 药物在有限的全身暴露下在便中达到高度,这表明药物在肠道中具有局部作用.
- ADS051具有作为一种安全有效的局部作用,针对中性粒细胞的治疗性结肠炎的潜力.
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