EVALUATION OF SAFETY AND EFFICACY OF 3TC (LAMIVUDINE) IN PATIENTS WITH ASYMPTOMATIC OR MILDLY SYMPTOMATIC HUMAN-IMMUNODEFICIENCY-VIRUS INFECTION - A PHASE I/II STUDY
EVALUATION OF SAFETY AND EFFICACY OF 3TC (LAMIVUDINE) IN PATIENTS WITH ASYMPTOMATIC OR MILDLY SYMPTOMATIC HUMAN-IMMUNODEFICIENCY-VIRUS INFECTION - A PHASE I/II STUDY
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DOI：
10.1093/infdis/171.5.1166
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发表时间：
1995-05-01
影响因子：
6.4
通讯作者：
DANNER, SA
中科院分区：
文献类型：
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作者：
VANLEEUWEN, R;KATLAMA, C;DANNER, SA
在一项I/II期研究中，在104例CD 4细胞计数≤ 400 × 10（6）/L的无症状和轻度症状的人类免疫缺陷病毒感染患者中研究了7种水平的3 TC治疗（0.5 - 20.0 mg/kg/d）。轻度和一过性腹泻、头痛、疲乏、恶心和腹痛是报告的最常见事件。未观察到剂量限制性毒性。在治疗的前4周内检测到CD 4细胞计数的小幅和一过性增加。随后在长期治疗期间进行性下降。在52周研究中观察到β 2-微球蛋白、新蝶呤和p24抗原水平持续降低，任何替代标志物均无一致的剂量-反应相关性，3 TC渗透入脑脊液（CSF）的范围与ddC和ddI报告的范围相同;平均CSF-血清比为0.06。这些发现表明，3 TC具有良好的安全性，并在研究剂量下具有抗逆转录病毒活性。
In a phase I/II study, 7 levels of 3TC therapy (from 0.5 to 20.0 mg/kg/day) were studied in 104 asymptomatic and mildly symptomatic human immunodeficiency virus-infected patients with CD4 cell counts less than or equal to 400 X 10(6)/L. Mild and transient episodes of diarrhea, headache, fatigue, nausea, and abdominal pain were the most frequent events reported. No dose-limiting toxicities were observed. Small and transient increases in CD4 cell counts were detected during the first 4 weeks of treatment. These were followed by progressive declines during prolonged therapy. Sustained decreases in beta(2)-microglobulin, neopterin, and p24 antigen levels were seen over the 52-week study, There was no consistent dose-response correlation for any surrogate marker, Penetration of 3TC into cerebrospinal fluid (CSF) was in the same range as reported for ddC and ddI; the mean CSF-to-serum ratio was 0.06. These findings indicate that 3TC exhibits an excellent safety profile and has antiretroviral activity at the dosages studied.