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

在本报告期间，我们完成了这项多中心试验， 共涉及四个地点的35名受试者。我们招募了七个人 在我们的网站上总共有两个人在报道期间完成了这项研究 句号。赞助商和调查人员共同决定400毫克 QID是需要评估的最高剂量，最终 计划的队列将不会以最高建议剂量(即800)进行研究 Mg QID)。该药耐受性良好，无严重不良反应。 药代动力学数据显示，剂量超过时，吸收明显饱和。 200 mg qid，在最高剂量下受试者的血浆浓度 洛布卡韦在4-6小时内超过CMV的体外ED50。一个 尿液中有显著但不完全的抗病毒反应 受试者在其他一些中心学习。

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.