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

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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.