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[依曲韦林用于治疗经验丰富的患者]

[Etravirine in highly treatment-experienced patients].

作者信息

Palter Daniel Podzamczer, Corbera Elena Ferrer, Tiraboschi Juan Manuel

机构信息

Hospital Universitari de Bellvitge, L'Hospitalet de Llobregat, Barcelona, España.

出版信息

Enferm Infecc Microbiol Clin. 2009 Dec;27 Suppl 2:6-11. doi: 10.1016/S0213-005X(09)73213-6.

Abstract

Etravirine (ETR) has demonstrated efficacy in patients with multiple prior treatments with prior virological failure and resistance mutations to various families of antiretroviral drugs. Most of the evidence concerning this drug has been drawn from the DUET studies, consisting of two multicenter, randomized, double-blind clinical trials with identical designs that included 1,200 patients. These trials showed that ETR obtained a superior virological and immunological response to placebo, reducing the incidence of hospital admissions and progression to AIDS/death. The most frequent adverse effect was rash, which was generally mild to moderate and required treatment discontinuation in only 2%. There were no differences in gastrointestinal, liver or lipid toxicities compared with the placebo arm. Because of the recent development of new drugs, effective regimens are now available for multi-treated patients. The TRIO study evaluated the efficacy and tolerability of one of the regimens most widely used today (ETR/raltegravir/darunavir/r) with excellent virological and immunological response (86% of viral load < 50 copies and CD4 +108 at 48 weeks) and excellent tolerance. ETR is effective and well tolerated and is the first non-nucleoside reverse transcriptase inhibitor (NNRTI) that allows the sequential use of drugs in this family, due to its high genetic barrier compared with firstgeneration NNRTI. Moreover, its long half-life allows once daily administration in patients requiring a QD regimen.

摘要

依曲韦林(ETR)已在接受过多种先前治疗且对各类抗逆转录病毒药物出现病毒学失败和耐药突变的患者中显示出疗效。关于这种药物的大部分证据来自DUET研究,该研究由两项设计相同的多中心、随机、双盲临床试验组成,纳入了1200名患者。这些试验表明,与安慰剂相比,依曲韦林获得了更好的病毒学和免疫学反应,降低了住院率以及进展为艾滋病/死亡的发生率。最常见的不良反应是皮疹,通常为轻度至中度,仅2%的患者需要停药。与安慰剂组相比,胃肠道、肝脏或脂质毒性方面没有差异。由于新药的近期研发,现在有了适用于多线治疗患者的有效方案。TRIO研究评估了当今使用最广泛的方案之一(依曲韦林/雷特格韦/达芦那韦/r)的疗效和耐受性,该方案具有出色的病毒学和免疫学反应(48周时86%的病毒载量<50拷贝且CD4 +108)以及出色的耐受性。依曲韦林有效且耐受性良好,由于与第一代非核苷类逆转录酶抑制剂(NNRTI)相比具有较高的基因屏障,它是首个允许在该类药物中序贯使用的非核苷类逆转录酶抑制剂。此外,其较长的半衰期允许在需要每日一次给药方案的患者中每日给药一次。

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