一种逆转录酶抑制剂3TC在HIV感染患者中的安全性和药代动力学：一项I期研究。
The safety and pharmacokinetics of a reverse transcriptase inhibitor, 3TC, in patients with HIV infection: a phase I study.
作者信息
van Leeuwen R, Lange J M, Hussey E K, Donn K H, Hall S T, Harker A J, Jonker P, Danner S A
机构信息
Department of Internal Medicine (AIDS Unit), Academic Medical Centre, University of Amsterdam, The Netherlands.
出版信息
AIDS. 1992 Dec;6(12):1471-5. doi: 10.1097/00002030-199212000-00008.
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.
目的
确定核苷类似物3TC的安全性和药代动力学。
设计
一项I期开放标签单中心研究。
方法
20名无症状、未接受过抗逆转录病毒治疗、CD4淋巴细胞计数<500×10⁶/l的HIV感染男性患者完成了该研究。每位患者先接受一次静脉给药，随后接受一次3TC口服给药。五个剂量水平（0.25、1.0、2.0、4.0和8.0mg/kg）各有4名患者给药。
结果
最常报告的不良事件是头痛，通常报告为轻度。口服给药后3TC的平均生物利用度为82%。大部分剂量（约70%）以原形经尿液排出。
结论
总体而言，给药后3TC耐受性良好，所测量的安全性参数无显著变化。正在进行3TC的I/II期临床试验以评估其安全性、药代动力学和初步活性。
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