LACK OF EFFECT OF CHOLESTEROL ESTERASE INHIBITOR CVT 1 ON CHOLESTEROL ABSORPTION

胆固醇酯酶抑制剂 CVT 1 对胆固醇吸收缺乏影响

• 批准号: 6665872
• 负责人: RICHARD E. OSTLUND
• 金额: $ 15.75万
• 依托单位: WASHINGTON UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-08-01 至 2003-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6665872
• 关键词: biological products; biomedical resource; drug /agent; proteins; spectrometry

. Two clinical trials were performed to test the hypothesis that CVT-1, a potent inhibitor of pancreatic cholesterol esterase, reduces percent cholesterol absorption and LDL cholesterol in humans. Measurements of cholesterol absorption were made with deuterated cholesterol tracers given orally and intravenously and detected in plasma by a new technique using negative ion mass spectrometry. Study 1 was a randomized, double-blind parallel study of CVT-1 treatment at doses of 0, 300, 1500, and 3000 mg/day in 19 subjects. Percent cholesterol absorption measured at baseline and again after 2 and 6 weeks showed no treatment effect and LDL cholesterol was unchanged. Study II was a randomized open-label crossover comparison between CVT-1 given as 1000 mg three times daily for 2 weeks and 187.5 mg hourly 16 hours/day for 2 weeks. Percent cholesterol absorption and plasma LDL cholesterol were not different between periods. We conclude that cholesterol esterase is not requir ed for unesterified cholesterol absorption in human subjects.

. 进行了两项临床试验来检验假设， CVT-1是一种有效的胰腺胆固醇酯酶抑制剂， 人体内胆固醇吸收率和低密度脂蛋白胆固醇。 胆固醇吸收的测量是用氘代 口服和静脉注射胆固醇示踪剂， 等离子体的新技术，使用负离子质谱。 研究 1是一项CVT-1治疗的随机、双盲平行研究， 19例受试者接受0、300、1500和3000 mg/天剂量。 百分 在基线时测量胆固醇吸收，并在第2和6天后再次测量 6周显示无治疗效果，LDL胆固醇无变化。 研究II是一项随机开放标签交叉比较， CVT-1以1000 mg每日三次给药，持续2周， 每小时16小时/天2周。 胆固醇吸收百分比， 血浆低密度脂蛋白胆固醇没有不同时期。 我们 结论是胆固醇酯酶是 人体吸收未酯化胆固醇不需要艾德 科目