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The safety and pharmacokinetics of a reverse transcriptase inhibitor, 3TC, in patients with HIV infection: a phase I
R van Leeuwen1, J M Lange, E K Hussey
1Department of Internal Medicine (AIDS Unit), Academic Medical Centre, University of Amsterdam, The Netherlands.
Objective:
To determine the safety and pharmacokinetics of the nucleoside analogue, 3TC.
Design:
A Phase I, open-label, single-centre study.
Methods:
Twenty asymptomatic, HIV-infected male patients with CD4 lymphocyte counts < 500 x 10(6)/l who had not received previous antiretroviral therapy completed the study. Each patient received a single intravenous dose followed by a single oral dose of 3TC. Four patients were dosed at each of five dose levels (0.25, 1.0, 2.0, 4.0 and 8.0 mg/kg).
Results:
The most commonly reported adverse event was headache, which was generally reported to be mild. The mean bioavailability of 3TC was 82% following oral administration. The majority of the dose (approximately 70%) was excreted unchanged in the urine.
Conclusions:
Overall, 3TC was well tolerated following dosing, and there were no significant changes in the safety parameters measured. Phase I/II clinical trials with 3TC are ongoing to evaluate its safety, pharmacokinetics and preliminary activity.