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: 6486752
• 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: 2001
• 资助国家: 美国
• 起止时间: 2001-08-01 至 2002-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6486752
• 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以下假设： CVT-1 是一种有效的胰腺胆固醇酯酶抑制剂，可降低 人体胆固醇吸收百分比和低密度脂蛋白胆固醇。 胆固醇吸收的测量是用氘代的 口服和静脉注射胆固醇示踪剂并在 等离子体通过使用负离子质谱的新技术。 学习 1 是一项 CVT-1 治疗的随机、双盲平行研究 19 名受试者每天服用 0、300、1500 和 3000 毫克的剂量。 百分比 在基线时以及 2 点和 6 点后再次测量胆固醇吸收 几周没有显示治疗效果，低密度脂蛋白胆固醇没有变化。 研究 II 是一项随机开放标签交叉比较 CVT-1 剂量为 1000 mg，每天 3 次，持续 2 周，然后服用 187.5 mg 每小时 16 小时/天，持续 2 周。 胆固醇吸收百分比和 不同时期的血浆低密度脂蛋白胆固醇没有差异。 我们 得出胆固醇酯酶是 人体吸收非酯化胆固醇不需要 科目。