在健康志愿者和患有吉尔伯特综合征的人群中,Faldaprevir的药理动力学和药理动力学
在PubMed上查看摘要
概括
此摘要是机器生成的。在健康男性和吉尔伯特综合征患者中,Faldaprevir (FDV) 是一种C型肝炎蛋白酶抑制剂,其暴露量呈剂量依赖的增加,并且耐受良好. 药物动力学是时间依赖的,在一周内达到稳定状态.
科学领域
- 肝病学
- 药理学
- 药物开发
背景情况
- 慢性型肝炎病毒 (HCV) 感染仍然是全球重要的健康问题.
- 在抗病毒治疗中,HCV NS3/4A蛋白酶抑制剂至关重要.
- 法尔达普雷维尔 (FDV) 是一种针对HCV的试验性蛋白酶抑制剂.
研究的目的
- 评估Faldaprevir多次增加剂量的安全性,耐受性和药理动力学 (PK).
- 在健康的男性志愿者和吉尔伯特综合征 (GS) 患者中评估FDV.
主要方法
- 在健康男性中进行随机,双盲,安慰剂控制的研究.
- 多次增加口服FDV (20- 240毫克) 或安慰剂剂.
- 在9名GS受试者中开放的FDV (240毫克) 持续28天.
- 单剂和多剂后的药理学和安全性评估.
主要成果
- FDV的暴露 (AUC,Cmax) 和时间依赖的PK的增加大于剂量.
- 平均半衰期 (t1/ 2) 为20至30小时;稳定状态在6至7天内实现.
- 在GS患者中,FDV暴露程度相似,但略低;总胆红素因剂量而增加.
- 在这两种群体中,FDV通常耐受性高达240mg/天.
结论
- 法尔达普雷维尔表现出非线性,时间依赖的药理动力学.
- 在高达240毫克/天的剂量下,FDV通常是安全的和耐受的.
- 药物的抗胰岛素特征支持在慢性型肝炎治疗中进行进一步的研究.
相关概念视频
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