MULTIPLE DOSE SAFETY, PHARMACOKINETICS, ANTIRETROVIRAL--BMS 180194 IN AIDS

艾滋病中的多剂量安全性、药代动力学、抗逆转录病毒药物 - BMS 180194

• 批准号: 6245473
• 负责人: BRENT G PETTY
• 金额: $ 2.23万
• 依托单位: JOHNS HOPKINS UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-03-05 至 1997-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6245473
• 关键词: AIDS therapy; antiviral agents; clinical research; dosage; drug screening /evaluation; drug tolerance; guanine analog; human subject; human therapy evaluation; pharmacokinetics; urinalysis

During this reporting period, we completed this multicenter trial, involving a total of 35 subjects at the four sites. We recruited seven subjects total at our site, two completing the study during this reporting period. The sponsor and investigators have jointly decided that 400 mg QID was the highest dose that needed to be assessed, and that the final planned cohort will not be studied at the highest proposed dose (i.e., 800 mg QID). The drug was tolerated well, without serious adverse events. Pharmacokinetic data showed apparently saturable absorption at dose over 200 mg QID, and at the highest doses the subjects' plasma concentrations of lobucavir exceeded the in vitro ED50 of CMV for 4-6 hours. A significant but incomplete antiviral response in urine was demonstrated in subjects studied at some of the other centers.

在本报告期内，我们完成了这项多中心试验， 共涉及四个研究中心的35名受试者。 我们招募了七个 我们研究中心共有2例受试者，在本报告期间完成了研究 期 申办者和研究者共同决定，400 mg QID是需要评估的最高剂量，并且最终剂量为 计划的队列将不在最高建议剂量下进行研究（即，800 mg QID）。 药物耐受性良好，无严重不良事件。 药代动力学数据显示，剂量超过 200 mg QID，最高剂量时受试者的血药浓度 Lobucavir的体外ED_（50）超过CMV的体外ED_（50）4-6小时。 一 尿中显示出显著但不完全的抗病毒反应， 在其他一些中心研究的对象。