多剂量cenerimod的药理动力学和木炭对其消除的影响
Markus S Mueller1, Pierre-Eric Juif1, Hakim Charfi2
1Department of Clinical Pharmacology, Idorsia Pharmaceuticals Ltd, Allschwil, Switzerland.
对于全身性红斑狼的治疗方法Cenerimod,它没有经历肠肝循环 (EHC). 活性炭在健康参与者中没有加速cenerimod的消除,这表明没有显著的EHC.
科学领域:
- 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:
- 塞内利莫德是一种用于治疗系统性红斑狼的试验性斯芬戈-1-酸盐受体1调节剂.
- 它的药理动力学特征表明,由于吸收缓慢和半衰期长,潜在的肠肝循环 (EHC) 可能发生.
研究的目的:
- 在健康参与者中研究cenerimod的潜在EHC.
- 评估活性炭是否可以加速cenerimod的消除.
- 评估cenerimod.com的多剂量药理动力学,药理动力学,安全性和耐受性.
主要方法:
- 健康的参与者每天接受口服cenerimod (0.5和4毫克) 50天.
- 用活性炭来评估其对cenerimod消除的影响.
- 监测了药理动力学和药理动力学参数,安全性和耐受性.
主要成果:
- 塞内利莫德显示吸收缓慢,消除多相,并显著的积累与延长半衰期 (大约. 30-33天) 的时间.
- 活性炭的使用没有显著改变cenerimod的终端半衰期,这表明没有实质性的EHC.
- 观察到淋巴细胞数量的可逆,剂量依赖的减少,没有发现安全问题.
结论:
- 塞内利莫德似乎没有经历显著的肠肝循环.
- 活性炭在加速cenerimod消除方面无效.
- 赛尼莫德表现出良好的安全性,并调节淋巴细胞数量,支持其对系统性红斑狼的持续发展.
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